Neratinib | HKI-272 | 来那替尼 (HKI-272) | Tyrosine / EGF Receptor Protein Kinase Inhibitor | EGFR | HER2

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Neratinib/来那替尼 {[allProObj[0].p_purity_real_show]}

货号：A150970 同义名： 来那替尼 (HKI-272) / HKI-272

Neratinib（HKI-272）是一种口服可用的、不可逆的、高度选择性的HER2和EGFR抑制剂，对其IC50值分别为59 nM和92 nM。

Neratinib/来那替尼化学结构
CAS号：698387-09-6

Neratinib/来那替尼 3D分子结构
CAS号：698387-09-6

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Neratinib/来那替尼纯度/质量文件产品仅供科研

货号：A150970 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

EGFR 亚型比较
HER2 亚型比较

产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750), IC50: 2 nM EGFR (E746_A750/T790M), IC50: 14 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKC,PKA	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		98%
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		98%
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					Src,VEGFR	98%
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						98%
AG 494	+ EGFR, IC50: 1.2 μM						99%+
AG-556	+ EGFR, IC50: 5 μM						98%
RG13022	+ EGFR, IC50: 4 μM						99%+
Tyrphostin RG 14620	✔						99%+
Vandetanib	+ EGFR, IC50: 500 nM						99%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		99%
AZD3759	++++ EGFR (WT), IC50: 0.3 nM EGFR (L858R), IC50: 0.2 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR (L861Q), IC50: 4 nM EGFR, IC50: 5 nM						99%+
AG1557	✔						99%
Rociletinib	++ EGFR (wt), Ki: 303.3 nM EGFR (L858R/T790M), Ki: 21.5 nM						98%
AG490	+ EGFR, IC50: 0.1 μM						98%
Cetuximab	++++ EGFR, Kd: 0.39 nM						95%
Osimertinib	++ WT EGFR, IC50: 12.92 nM L858R/T790M EGFR, IC50: 11.44 nM						98%
Osimertinib mesylate	✔						98% (Content MsOH 15.2-18.2%)
Chrysophanol	✔					mTOR	98%
PD153035	++++ EGFR, Ki: 5.2 pM						99%+
Olmutinib	✔					BTK	99%+
WZ4002	++++ EGFR (L858R/T790M), IC50: 8 nM EGFR (L858R), IC50: 2 nM						99%+
Icotinib	+++ EGFR, IC50: 5 nM						99%
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						98%
Cyasterone	✔						99%+
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						98%
WZ8040	✔						99%+
(-)-Epigallocatechin Gallate	✔						99%
AG 18	+ EGFR, IC50: 35 μM						99%+
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						99%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L861Q) , IC50: <1 nM EGFR (L858R), IC50: 6 nM		+++ ErbB4, IC50: 7 nM			BRK	99%+
Butein	✔						95%
Genistein	✔						98%
SU5214	+ EGFR, IC50: 36.7 μM						99%+
Naquotinib	✔						99%+
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		98%
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		99%
Lazertinib	++++ WT EGFR, IC50: 76 nM L858R/T790M EGFR, IC50: 2 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	98%
(E)-AG 99	✔						99%+
Licochalcone D	✔					Caspase,PARP	99%
Zipalertinib	+++ EGFR (L861Q), IC50: 4.1 nM EGFR WT, IC50: 8 nM		+++ HER4, IC50: 4 nM		++++ EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 nM		97%
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		99%+
Firmonertinib mesylate	✔						99%+
Tyrphostin AG30	✔						99%+
EGFR-IN-12	++ EGFR, IC50: 21 nM						99%+
Mobocertinib	✔						98%
(Rac)-JBJ-04-125-02	✔						95%
(S)-Sunvozertinib	✔						99%
BLU-945	✔						95%
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			98%
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			99%+
ARRY-380 analog				✔			99%
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			99%+
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			98%
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			99%+
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			95%
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			98%
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms/CSF1R	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^L858R/T790M, IC50: 0.51 nM EGFR^T790M, IC50: 0.79 nM		98+%
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	98%
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			98%
Tucatinib				+++ ErbB2, IC50: 8 nM			98%
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Src,Raf	99%+
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			99%+
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	99%+
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			99%+
Afatinib dimaleate	++++ EGFR (wt), IC50: 0.5 nM EGFR (L858R/T790M), IC50: 0.4 nM			++ HER2, IC50: 14 nM			98%
Canertinib 2HCl	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			99%
Allitinib tosylate	++++ EGFR (T790M/L858R), IC50: 12 nM EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			97%
Afatinib	++++ EGFR (wt), IC50: 0.5 nM EGFR (L858R), IC50: 10 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			99%
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			98%
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			99%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			99%
ALK-IN-1					++ EGFR(C797S/del19), IC50: 138.6 nM EGFR(del19), IC50: 36.8 nM	ALK	99%
Brigatinib					+ EGFR(C797S/T790M/del19), IC50: 67.2 nM EGFR(del19), IC50: 39.9 nM	ALK,FLT3	98%
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	99%+
EAI045					✔		97%
Almonertinib					✔		99%
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^L858R/T790M, IC50: 0.19 nM EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	HER2 ↓ ↑	其他靶点	纯度
Poziotinib	++++ HER2, IC50: 5.3 nM		98%
Tyrphostin AG 879	+ HER2-Neu, IC50: 1.0 μM		95%
TAK-285	+ HER2, IC50: 17 nM		99%+
ARRY-380 analog	✔		99%
Canertinib	+++ ErbB2, IC50: 9.0 nM	EGFR	99%+
(E/Z)-CP-724714	++ HER2/ErbB2, IC50: 10 nM		95%
Lapatinib	+++ ErbB2, IC50: 9.2 nM	EGFR	98%
AEE788	++++ HER2/ErbB2, IC50: 6 nM	EGFR	98+%
Neratinib	+ HER2, IC50: 59 nM	EGFR,Src	98%
BMS-599626	+ HER2, IC50: 30 nM		98%
Mubritinib	++++ HER2/ErbB2, IC50: 6.0 nM		99%+
Tucatinib	+++ ErbB2, IC50: 8 nM		98%
Sapitinib	++++ ErbB2, IC50: 3 nM	EGFR	99%+
CUDC-101	++ HER2, IC50: 15.7 nM	EGFR,HDAC	99%+
Afatinib dimaleate	++ HER2, IC50: 14 nM		98%
Afatinib	++ HER2, IC50: 14 nM		99%
Pertuzumab	✔		95%
Trastuzumab	✔		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Neratinib/来那替尼生物活性

靶点	EGFR/ErbB1 EGFR, IC50:92 nM HER2/ErbB2 HER2, IC50:59 nM HER2 HER2, IC50:59 nM
描述	Deregulated expression of receptors EGFR and HER2, two closely related members of the ErbB family of transmembrane receptor tyrosine kinases, has been implicated in the development and malignancy of numerous types of human cancers, making them become a potential target for therapy. Neratinib is a potent inhibitor of HER2 and EGFR with IC50 values of 59nM and 92nM (measured by an autophosphorylation assay using time-resolved fluorometry), respectively. Neratinib>10nM could inhibit autophosphorylation of HER2 in BT474 cells treated for 3h, and EGF-induced autophosphorylation of EGFR in A431. Cell viability assays showed that Neratinib could inhibit HER-2-overexpressing breast cancer cell lines, SK-Br-3 and BT474, with low IC50 values (2nM), as well as EGFR-overexpressed cell line with IC50 value of 81nM, but exhibited much less activation on EGFR- and HER-2-negative cell lines, MDA-MB-435 and SW620. For activation of HER2 can lead to activation of both MAPK pathway and the Akt signal transduction pathways, a test for Neratinib on this two pathway has been done. Neratinib at concentration>2nM caused decreased level of both p-MAPK and p-AKT in BT474 cells. Treatment with Neratinib at concentration>5nM for 12-16h also led to decrease of cyclin D1 and retinoblastoma (Rb), as well as increased p27 in BT474, suggesting the cell cycle block by Neratinib. Oral administration of Neratinib at dose ranging in 10-80mg/kg exhibited anti-tumor activity against various tumor models, including 3T3/neu cells, BT474, SK-OV-3, A431 and MCF-7 xenografts^[1].
作用机制	Neratinib binds irreversibly to the ATP binding pocket of HER member receptor tyrosine kinases.^[2]

Neratinib/来那替尼细胞实验

Cell Line MDA-MB-453 MDA-MB-361 HCC-1954 BT-474 SK-BR-3 TBCP-1 cells SKBR3 cells SKBR-3 cells Pancreatic cancer cells T cell lymphoma cells INS-1E cells Human islet cells HCC1954 HCC1569 JIMT-1 HME2-parental cells	Concentration	Treated Time	Description	References
MDA-MB-453	10 nM	24 hours	Neratinib monotherapy significantly inhibited cell viability, and its combination with trastuzumab was even more effective.	Br J Cancer. 2024 Jun;130(12):1990-2002.
MDA-MB-361	10 nM	24 hours	Neratinib monotherapy significantly inhibited cell viability, and its combination with trastuzumab was even more effective.	Br J Cancer. 2024 Jun;130(12):1990-2002.
HCC-1954	1 µM	24 hours	To evaluate the synergistic effects of Neratinib with mTOR inhibitors, MEK inhibitors, PI3K α inhibitors, and CDK4/6 inhibitors in HER2+ cells. Results showed that Neratinib exhibited significant synergistic anti-proliferative effects with these inhibitors in HCC-1954 cells.	Clin Cancer Res. 2021 Mar 15;27(6):1681-1694.
BT-474	25 nM	24 hours	To evaluate the synergistic effects of Neratinib with mTOR inhibitors, MEK inhibitors, PI3K α inhibitors, and CDK4/6 inhibitors in HER2+ cells. Results showed that Neratinib exhibited significant synergistic anti-proliferative effects with these inhibitors in BT-474 cells.	Clin Cancer Res. 2021 Mar 15;27(6):1681-1694.
SK-BR-3	10 nM	24 hours	To evaluate the synergistic effects of Neratinib with mTOR inhibitors, MEK inhibitors, PI3K α inhibitors, and CDK4/6 inhibitors in HER2+ cells. Results showed that Neratinib exhibited weaker synergistic anti-proliferative effects with these inhibitors in SK-BR-3 cells.	Clin Cancer Res. 2021 Mar 15;27(6):1681-1694.
TBCP-1 cells	300 nM	24 hours	To investigate the effect of Neratinib on the transcriptome of TBCP-1 cells, it was found that Neratinib induced ferroptosis	Breast Cancer Res. 2019 Aug 13;21(1):94.
SKBR3 cells	5 nM	24 hours	To investigate the effect of Neratinib on SKBR3 cells, it was found that Neratinib induced ferroptosis	Breast Cancer Res. 2019 Aug 13;21(1):94.
SKBR-3 cells	45 to 250 ng/mL	48 hours	To evaluate the antiproliferative activity of Neratinib and its nanoformulations on SKBR-3 cells. The results showed that Neratinib-loaded dendrimers were more cytotoxic than Neratinib alone, and Trastuzumab-grafted Neratinib dendrimers were more cytotoxic than non-grafted Neratinib dendrimers.	Int J Nanomedicine. 2020 Jul 30;15:5433-5443.
Pancreatic cancer cells	50 nM	6 hours	Neratinib reduced the phosphorylation of PAK1, Ezrin, and Merlin, and increased the phosphorylation of MAP4K4.	J Cell Physiol. 2020 Nov;235(11):7889-7899.
T cell lymphoma cells	50 nM	6 hours	Neratinib reduced MST4 expression and Ezrin T567 phosphorylation.	J Cell Physiol. 2020 Nov;235(11):7889-7899.
INS-1E cells	5 µM and 10 µM	72 hours	Neratinib potently inhibited H2O2- and high glucose/palmitate-induced MST1 activation and apoptosis, and restored PDX1 expression.	Nat Commun. 2019 Nov 1;10(1):5015.
Human islet cells	10 µM and 25 µM	72 hours	Neratinib significantly inhibited pro-inflammatory cytokine- and high glucose/palmitate-induced MST1 activation and caspase-3 activation.	Nat Commun. 2019 Nov 1;10(1):5015.
HCC1954	150 nM	twice weekly	To evaluate the synergistic anti-proliferative effect of Neratinib and Dasatinib, results showed that the combination was more effective than single agents in inhibiting cell proliferation	Transl Oncol. 2024 Nov;49:102073.
HCC1569	150 nM	twice weekly	To evaluate the synergistic anti-proliferative effect of Neratinib and Dasatinib, results showed that the combination was more effective than single agents in inhibiting cell proliferation	Transl Oncol. 2024 Nov;49:102073.
JIMT-1	150 nM	twice weekly	To evaluate the synergistic anti-proliferative effect of Neratinib and Dasatinib, results showed that the combination was more effective than single agents in inhibiting cell proliferation	Transl Oncol. 2024 Nov;49:102073.
HME2-parental cells	1 µM		To evaluate the inhibitory effect of neratinib on HER2 phosphorylation	Mol Biomed. 2022 Jun 22;3(1):19.

Neratinib/来那替尼动物实验

Species Nude mice Mice NSG mice Mice Mice Female Albino Wistar rats BALB/C mice BALB/c Nude mice	Animal Model Patient-derived xenograft (PDX) models HER2-positive breast cancer xenograft models Breast cancer model CW2 xenograft model Type 1 diabetes (streptozotocin-induced) and type 2 diabetes (obese Leprdb/db) mouse models Neratinib-induced diarrhea model TBCP-1 spontaneous brain metastasis model HCC1954 xenograft model	Administration	Dosage	Frequency	Description	References
Nude mice	Patient-derived xenograft (PDX) models	Oral	10 mg/kg	Daily for the duration of the experiment	To evaluate the antitumor efficacy of Neratinib in combination with CDK4/6 inhibitors, mTOR inhibitors, and MEK inhibitors in HER2+ PDX models. Results showed that the combination of Neratinib with palbociclib significantly enhanced antitumor efficacy in all five PDX models, while combinations with everolimus or trametinib showed varying therapeutic benefits across different models.	Clin Cancer Res. 2021 Mar 15;27(6):1681-1694.
Mice	HER2-positive breast cancer xenograft models	Oral	20 mg/kg	5 days/week, continued treatment	To evaluate the efficacy of Neratinib in combination with Trastuzumab, results showed that Neratinib plus Trastuzumab was superior to Pertuzumab plus Trastuzumab in accelerating tumor regression and complete response	NPJ Breast Cancer. 2021 May 27;7(1):63
NSG mice	Breast cancer model	Oral gavage	27 mg/kg	Every other day until tumors reached 1000 mm³	To evaluate the effect of neratinib on tumor growth	Mol Biomed. 2022 Jun 22;3(1):19.
Mice	CW2 xenograft model	Oral	40 mg/kg neratinib, 40 mg/kg alpelisib	Once daily for 14 days	To test the therapeutic effect of neratinib and alpelisib combination on CW2 xenograft model.	Cancer Cell. 2021 Aug 9;39(8):1099-1114.e8
Mice	Type 1 diabetes (streptozotocin-induced) and type 2 diabetes (obese Leprdb/db) mouse models	Intraperitoneal injection	5 mg/kg	Once daily for 35 days (type 1 diabetes model) and 31 days (type 2 diabetes model)	Neratinib significantly attenuated hyperglycemia and improved β-cell function, survival, and β-cell mass.	Nat Commun. 2019 Nov 1;10(1):5015.
Female Albino Wistar rats	Neratinib-induced diarrhea model	Oral gavage	50 mg/kg	Once daily for 28 days	To investigate the effect of antibiotics on neratinib-induced diarrhea. Results showed that rats treated with vancomycin or neomycin had significantly lower levels of diarrhea than rats treated with neratinib alone, while the broad-spectrum antibiotic cocktail was less effective.	Neoplasia. 2022 Aug;30:100806
BALB/C mice	TBCP-1 spontaneous brain metastasis model	Oral	60 mg/kg	Once daily for 3 weeks	To evaluate the efficacy of Neratinib in neoadjuvant therapy, it was found that Neratinib significantly inhibited tumor growth and brain metastasis, and prolonged survival	Breast Cancer Res. 2019 Aug 13;21(1):94.
BALB/c Nude mice	HCC1954 xenograft model	Oral	Neratinib 10 mg/kg, Dasatinib 15 mg/kg	5 days per week for 10 weeks	To evaluate the in vivo anti-tumor effect of Neratinib and Dasatinib, results showed that the combination had a prolonged anti-tumor effect compared to single agents	Transl Oncol. 2024 Nov;49:102073.

Neratinib/来那替尼动物研究

Dose

Rat^[3] (p.o.): 5 mg/kg - 100 mg/kg

Administration

p.o.

Pharmacokinetics

Animal	Rats^[3]	Dogs^[3]
Dose	10 mg/kg	2 mg/kg (male)
Administration	p.o.	p.o.
C_max	1.44 μg/ml	35.1 μg/ml
AUC_0→t	15.6 ng·hr/ml	323 ng·hr/ml

Neratinib/来那替尼临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02396108	Breast Cancer	Phase 1 Phase 2	Recruiting	March 2019	Singapore ... 展开 >> National University Hospital Recruiting Singapore, Singapore, 119228 Contact: Soo Chin Lee (65) 6779 5555 收起 <<
NCT03182634	Advanced Breast Cancer	Phase 2	Recruiting	November 2023	United Kingdom ... 展开 >> Royal Marsden Hosital, Sutton Recruiting Surrey, England, United Kingdom, SM2 5PT Royal Bournemouth Hospital Recruiting Bournemouth, United Kingdom Addenbrooke's Hospital Recruiting Cambridge, United Kingdom Royal Devon and Exeter Hospital Recruiting Exeter, United Kingdom Beatson West of Scotland Cancer Centre Recruiting Glasgow, United Kingdom Royal Marsden Hospital Recruiting London, United Kingdom University College Hospital London Recruiting London, United Kingdom Christie Hospital Recruiting Manchester, United Kingdom 收起 <<
NCT00366600	Healthy	Phase 1	Completed	-	United States, Washington ... 展开 >> Northwest Kinetics Tacoma, Washington, United States, 98418 收起 <<

Neratinib/来那替尼参考文献

[1]Rabindran SK, Discafani CM, et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 2004 Jun 1;64(11):3958-65.

[2]Feldinger K, Kong A, et al. Profile of neratinib and its potential in the treatment of breast cancer. Breast Cancer (Dove Med Press). 2015 Jun 9;7:147-62.

[3]208051Orig1s000

Neratinib/来那替尼实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

8.98mL

1.80mL

0.90mL

17.95mL

3.59mL

1.80mL

Neratinib/来那替尼技术信息

CAS号	698387-09-6
分子式	C₃₀H₂₉ClN₆O₃
分子量	557.04
SMILES Code	O=C(NC1=C(OCC)C=C2N=CC(C#N)=C(NC3=CC=C(OCC4=NC=CC=C4)C(Cl)=C3)C2=C1)/C=C/CN(C)C
MDL No.	MFCD09752958

别名	来那替尼 (HKI-272) ;HKI-272
运输	蓝冰
InChI Key	JWNPDZNEKVCWMY-VQHVLOKHSA-N
Pubchem ID	9915743

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 12 mg/mL(21.54 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

配制的工作液建议现用现配，短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02396108	Breast Cancer	Phase 1 Phase 2	Recruiting	March 2019	Singapore ... 展开 >> National University Hospital Recruiting Singapore, Singapore, 119228 Contact: Soo Chin Lee (65) 6779 5555 收起 <<
NCT03182634	Advanced Breast Cancer	Phase 2	Recruiting	November 2023	United Kingdom ... 展开 >> Royal Marsden Hosital, Sutton Recruiting Surrey, England, United Kingdom, SM2 5PT Royal Bournemouth Hospital Recruiting Bournemouth, United Kingdom Addenbrooke's Hospital Recruiting Cambridge, United Kingdom Royal Devon and Exeter Hospital Recruiting Exeter, United Kingdom Beatson West of Scotland Cancer Centre Recruiting Glasgow, United Kingdom Royal Marsden Hospital Recruiting London, United Kingdom University College Hospital London Recruiting London, United Kingdom Christie Hospital Recruiting Manchester, United Kingdom 收起 <<
NCT00366600	Healthy	Phase 1	Completed	-	United States, Washington ... 展开 >> Northwest Kinetics Tacoma, Washington, United States, 98418 收起 <<
NCT00380328	Healthy	Phase 1	Completed	-	-
NCT00708903	Breast Cancer	Phase 1	Completed	-	United States, Washington ... 展开 >> Tacoma, Washington, United States, 98418 收起 <<
NCT00550212	Healthy	Phase 1	Completed	-	-
NCT01042379	Breast Neoplasms ... 展开 >> Breast Cancer Breast Tumors 收起 <<	Phase 2	Recruiting	-	-
NCT02977780	Glioblastoma	Phase 2	Recruiting	May 2021	United States, Alabama ... 展开 >> University of Alabama at Birmingham Not yet recruiting Birmingham, Alabama, United States, 35294 Contact: L. Burt Nabors, MD 205-934-1432 bnabors@uab.edu United States, Massachusetts Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Isabel Arrillaga-Romany, MD PhD 617-724-8770 iarrillaga@mgh.harvard.edu Principal Investigator: Isabel Arrillaga-Romany, MD PhD Dana Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02115 Contact: Brian Alexander, MD MPH 617-732-7560 Brian_Alexander@dfci.harvard.edu Contact: Lisa Doherty, NP 617-632-2166 lisa_doherty@dfci.harvard.edu Principal Investigator: Brian Alexander, MD MPH United States, Minnesota Mayo Clinic Not yet recruiting Rochester, Minnesota, United States, 55905 Contact: Eva Galanis, MD 507-284-2511 galanis.evanthia@mayo.edu United States, New York Columbia University Medical Center Recruiting New York, New York, United States, 10032 Contact: Mary Welch, MD 212-342-0571 mw2517@cumc.columbia.edu United States, Ohio Cleveland Clinic Recruiting Cleveland, Ohio, United States, 44195 Contact: Manmeet Ahluwalia,, MD 216-444-6145 ahluwam@ccf.org United States, Pennsylvania University of Pittsburgh Medical Center Recruiting Pittsburgh, Pennsylvania, United States, 15232 Contact: Jan Drappatz, MD 412-864-7791 drappatzj@upmc.edu United States, Texas UT MD Anderson Cancer Center Not yet recruiting Houston, Texas, United States, 77030 Contact: John DeGroot, MD 713-745-3072 jdegroot@mdanderson.org United States, Utah Huntsman Cancer Institute Recruiting Salt Lake City, Utah, United States, 84112 Contact: Howard Colman, MD 801-587-4042 Howard.colman@hci.utah.edu United States, Virginia University of Virginia Health System Recruiting Charlottesville, Virginia, United States, 22908 Contact: David Schiff, MD 434-924-5610 Ds4jd@virginia.edu 收起 <<
NCT00757809	Healthy Subjects	Phase 1	Completed	-	United States, Texas ... 展开 >> Austin, Texas, United States, 78752 United States, Washington Tacoma, Washington, United States, 98418 收起 <<
NCT00498745	Healthy	Phase 1	Completed	-	United States, Texas ... 展开 >> San Antonio, Texas, United States, 78217 收起 <<
NCT00146172	-		Completed	-	-
NCT00768469	Advanced Malignant Solid Tumor... 展开 >>s 收起 <<	Phase 1	Completed	-	Japan ... 展开 >> Investigational Site Shizuoka, Japan Investigational Site Tokyo, Japan 收起 <<
NCT00397046	-		Completed	-	-
NCT01494662	Breast Cancer	Phase 2	Recruiting	December 2023	United States, California ... 展开 >> University of California, San Francisco Medical Center Active, not recruiting San Francisco, California, United States, 94115 United States, District of Columbia MedStar Georgetown Univeristy Hospital Active, not recruiting Washington, District of Columbia, United States, 20007 United States, Maryland Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Active, not recruiting Baltimore, Maryland, United States, 21231 United States, Massachusetts Beth Israel Deaconess Medical Center Active, not recruiting Boston, Massachusetts, United States, 02215 Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Rachel Freedman, MD Principal Investigator: Rachel Freedman, MD, MPH Massachusetts General Hosptial Recruiting Boston, Massachusetts, United States, 02215 Contact: Beverly Moy, MD Principal Investigator: Beverly Moy, MD United States, Michigan University of Michigan Comprehensive Cancer Center Active, not recruiting Ann Arbor, Michigan, United States, 48109 United States, North Carolina University of North Carolina at Chapel Hill - Lineberger Comprehensive Cancer Center Active, not recruiting Chapel Hill, North Carolina, United States, 27599 Duke University Medical Center Active, not recruiting Durham, North Carolina, United States, 27710 United States, Pennsylvania UPMC Cancer Centers - Magee-Womens Hospital of UPMC Active, not recruiting Pittsburgh, Pennsylvania, United States, 15213 United States, Texas Baylor College of Medicine Lester and Sue Smith Breast Center Active, not recruiting Houston, Texas, United States, 77030 MD Anderson Cancer Center Active, not recruiting Houston, Texas, United States, 77030 收起 <<
NCT00398567	Advanced Breast Cancer	Phase 1 Phase 2	Completed	-	United States, California ... 展开 >> City of Hope National Medical Center Duarte, California, United States, 91010-3000 LAC/USC Medical Center, USC/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 City of Hope National Medical Center Pasadena, California, United States, 91105 United States, Maryland University of Maryland, University of Maryland Medical Center Baltimore, Maryland, United States, 21201 United States, North Carolina Duke University, Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Pennsylvania Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 China, Jiangsu Chinese Nanjing Bayi Hospital Nanjing, Jiangsu, China, 210002 China, Tianjin Tianjin Union Medicine Center Tianjin, Tianjin, China, 300121 China Cancer Hospital, Academy of Med Science and Peking Union Med Beijing, China, 100021 307 Hospital of Chinese People's Liberation Army Beijing, China, 100071 Chinese PLA General Hospital Beijing, China, 100853 France Institut Curie Paris, France, 75005 Centre Rene Gauducheau Saint-Herblain, France, 44805 Switzerland Centre Hospitalier Universitaire Vaudois Lausanne, Switzerland, CH-1011 收起 <<
NCT00398567	-		Completed	-	-
NCT00768469	-		Completed	-	-
NCT01008150	Breast Cancer	Phase 2	Completed	-	-
NCT00146172	Breast Neoplasms	Phase 1	Completed	-	United States, Florida ... 展开 >> H. Lee Moffitt Cancer Center & Research Institute Tampa, Florida, United States, 33612 United States, Massachusetts Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, Ohio The Cleveland Clinic Foundation Taussig Cancer Center Cleveland, Ohio, United States, 44195 United States, Tennessee The Sarah Cannon Cancer Center Nashville, Tennessee, United States, 37203 收起 <<
NCT02593708	Solid Tumor	Phase 1	Terminated(toxicity)	-	United States, California ... 展开 >> UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94115 收起 <<
NCT01008150	-		Completed	-	-
NCT00777101	Advanced Breast Cancer ... 展开 >> Breast Cancer 收起 <<	Phase 2	Completed	-	-
NCT00397046	Tumors	Phase 1	Completed	-	Japan ... 展开 >> The Cancer Institute Hospital of Japanese Foundation for Cancer Research Koto, Tokyo, Japan, 135-8550 Shizuoka Cancer Center Shizuoka, Japan, 1411-8777 收起 <<
NCT00860223	Healthy	Phase 1	Completed	-	United States, Florida ... 展开 >> Miami, Florida, United States, 33126 收起 <<
NCT00777101	-		Completed	-	-
NCT00814060	Healthy Subjects	Phase 1	Completed	-	United States, Washington ... 展开 >> Tacoma, Washington, United States, 98418 收起 <<
NCT01670877	Breast Neoplasms	Phase 2	Recruiting	November 30, 2020	United States, Alabama ... 展开 >> University of Alabama Cancer Center Recruiting Birmingham, Alabama, United States, 35294 Contact: Andres Forero-Torres, M.D. 205-975-2837 aforero@uab.edu Principal Investigator: Andres Forero, M.D. United States, California University of Southern California Keck School of Medicine Recruiting Los Angeles, California, United States, 90033 Contact: Janice Lu, M.D., Ph.D. 323-865-3000 janice.lu@med.usc.edu Principal Investigator: Janice Lu, M.D., Ph.D. Stanford Medicine Cancer Institute Recruiting Stanford, California, United States, 94305 Contact: Mark Pegram, M.D. 650-723-5801 mpegram@stanford.edu Principal Investigator: Mark Pegram, M.D. United States, Florida University of Miami Hospital and Clinics Recruiting Miami, Florida, United States, 33136 Contact: Marc E Lippman, M.D. mlippman@med.miami.edu Principal Investigator: Marc E Lippman, M.D. Sub-Investigator: Carmen Calfa, M.D. Sub-Investigator: Mohammad Jahanzeb, M.D. Sub-Investigator: Judith Hurley, M.D. Sub-Investigator: Frances Valdes-Albini, M.D. Sub-Investigator: Lawrence Negret, M.D. Sub-Investigator: Reshma Mahtani, M.D. Sub-Investigator: Catherine Welsh, M.D. Sub-Investigator: Alejandra Perez, M.D. Sub-Investigator: Joyce Slingerland, M.D. Sub-Investigator: Charles Vogel, M.D. United States, Illinois Northwestern University - Feinberg School of Medicine Recruiting Chicago, Illinois, United States, 60611 Contact: Massimo Cristofanilli, M.D. 312-695-6180 massimo.cristofanilli@nm.org Principal Investigator: Massimo Cristofanilli, M.D. Sub-Investigator: William Gradishar, M.D. Sub-Investigator: Lisa Flaum, M.D. Rush University Medical Center Recruiting Chicago, Illinois, United States, 60612 Contact: Melody Cobleigh, M.D. melody_cobleigh@rush.edu Principal Investigator: Melody Cobleigh, M.D. United States, Massachusetts Dana-Farber Cancer Institute, Harvard University Recruiting Boston, Massachusetts, United States, 02215 Contact: Rachel Freedman, M.D. 617-632-6876 rachel_freedman@dfci.harvard.edu Principal Investigator: Rachel Freedman, M.D. United States, Michigan University of Michigan Active, not recruiting Ann Arbor, Michigan, United States, 48109 United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Matthew P. Goetz, M.D. 507-293-1605 Goetz.Matthew@mayo.edu Principal Investigator: Matthew P. Goetz, M.D. United States, Missouri St. Luke's Cancer Institute Recruiting Kansas City, Missouri, United States, 64111 Contact: Timothy J Pluard, M.D. 816-932-6005 tpluard@saint-lukes.org Principal Investigator: Timothy J Pluard, M.D. Washington University School of Medicine Recruiting Saint Louis, Missouri, United States, 63110 Contact: Cynthia Ma, M.D., Ph.D. 314-362-9383 cynthiaxma@wustl.edu Principal Investigator: Cynthia X Ma, M.D., Ph.D. Sub-Investigator: Michael Naughton, M.D. Sub-Investigator: Rama Suresh, M.D. Sub-Investigator: Foluso Ademuyiwa, M.D. Sub-Investigator: Leonel Hernandez-Aya, M.D. Sub-Investigator: Ron Bose, M.D., Ph.D. Sub-Investigator: Katherine Weilbaecher, M.D. Sub-Investigator: Ashley Frith, M.D. Sub-Investigator: Haeseong Park, M.D. Sub-Investigator: Matthew Cherian, M.D. Sub-Investigator: Lindsay Peterson, M.D. United States, North Carolina University of North Carolina at Chapel Hill (Lineberger Comprehensive Cancer Center) Recruiting Chapel Hill, North Carolina, United States, 27514 Contact: Carey Anders, M.D. 919-966-4431 canders@med.unc.edu Principal Investigator: Carey Anders, M.D. Sub-Investigator: E. Claire Dees, M.D. Sub-Investigator: Francis A. Collichio, M.D. Sub-Investigator: Trevor A. Jolly, M.D. Sub-Investigator: Katherine Reeder-Hays, M.D. Duke Cancer Institute at Duke University Medical Center Recruiting Durham, North Carolina, United States, 27710 Contact: Kimberly Blackwell, M.D. 919-681-0874 kimberly.blackwell@duke.edu Principal Investigator: Kimberly Blackwell, M.D. United States, South Dakota Avera Cancer Institute Recruiting Sioux Falls, South Dakota, United States, 57105 Contact: Amy Krie, M.D. 605-322-6900 amy.krie@avera.org Principal Investigator: Amy Krie, M.D. United States, Texas Baylor College of Medicine Recruiting Houston, Texas, United States, 77030 Contact: Julie Nangia, M.D. 713-798-1999 nangia@bcm.edu Principal Investigator: Julie Nangia, M.D. Sub-Investigator: Matthew JC Ellis, MB, Ph.D. Canada, British Columbia BC Cancer Agency Active, not recruiting Vancouver, British Columbia, Canada, V5Z 1L3 Canada, Ontario Princess Margaret Cancer Centre Active, not recruiting Toronto, Ontario, Canada, M5G 2M9 收起 <<
NCT00266877	Carcinoma, Non-Small-Cell Lung... 展开 >> Lung Neoplasms 收起 <<	Phase 2	Completed	-	United States, California ... 展开 >> USC Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, Illinois Midwestern Regional Medical Center Zion, Illinois, United States, 60099 United States, Massachusetts Massachusetts General Hospital, Yawkey Center for Outpatient Care Boston, Massachusetts, United States, 02114 United States, Minnesota University of Minnesota Minneapolis, Minnesota, United States, 55455 United States, New York Memorial Sloan-Kettering New York, New York, United States, 10021 United States, North Carolina Carolinas Hematology-Oncology Associates Charlotte, North Carolina, United States, 28203 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 Cleveland Clinic Cleveland, Ohio, United States, 44195 United States, Tennessee Vanderbilt University Medical Center Nashville, Tennessee, United States, 37232-6868 United States, Washington Swedish Cancer Institute Seattle, Washington, United States, 98104 Seattle Cancer Care Alliance Seattle, Washington, United States, 98109 France Institut Gustave Roussy Villejuif, France, 94805 Hungary Országos Korányi TBC és Pulmonológiai Intézet Budapest, Hungary, H-1529 University of Debrecen Debrecen, Hungary, H-4012 Poland Akademia Medyczna W Gdansku Gdansk, Poland, 80-952 Mazowieckie Centrum Leczenia Chorób Płuc i Gruźlicy Otwock, Poland, 05-400 Wielkopolskie Centrum Chorób Płuc i Gruźlicy Poznan, Poland, 60-569 Dolnośląskie Centrum Chorób Płuc we Wrocławiu Wrocław, Poland, 54-439 Spain Hospital Germans Trias I Puyol Badalona, Barcelona, Spain, 08916 收起 <<
NCT00932464	Healthy	Phase 1	Withdrawn(Study withdrawn as i... 展开 >>t no longer is deemed necessary per project status.) 收起 <<	August 2012	-
NCT00915018	-		Completed	-	-
NCT00915018	Breast Cancer	Phase 2	Completed	-	-
NCT00706030	Breast Cancer ... 展开 >> Advanced Malignant Solid Tumors 收起 <<	Phase 1 Phase 2	Completed	-	-
NCT00706030	-		Completed	-	-
NCT01423123	Breast Cancer	Phase 1	Completed	-	United States, New Jersey ... 展开 >> Cancer Institute of New Jersey New Brunswick, New Jersey, United States, 08901 United States, Pennsylvania NSABP Foundation, Inc. Pittsburgh, Pennsylvania, United States, 15212 University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15232-1305 United States, West Virginia West Virginia University Hospitals Morgantown, West Virginia, United States, 26506-9162 收起 <<
NCT00266877	-		Completed	-	-
NCT00445458	Advanced Breast Cancer ... 展开 >> Advanced Malignant Solid Tumors Breast Neoplasms 收起 <<	Phase 1 Phase 2	Completed	-	-
NCT00445458	-		Completed	-	-
NCT00838539	Neoplasms Mal... 展开 >>ignant Carcinoma 收起 <<	Phase 1	Completed	-	United States, Massachusetts ... 展开 >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02115 Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 Dana Farber Cancer Institute Boston, Massachusetts, United States, 02215 France Institut Gustave Roussy Villejuif, France, 94805 收起 <<
NCT00864487	Healthy Subjects	Phase 1	Completed	-	United States, Florida ... 展开 >> Miami, Florida, United States, 33126 收起 <<
NCT01956253	-		-	-	United States, North Carolina ... 展开 >> North Carolina Cancer Hospital (UNC) Chapel Hill, North Carolina, United States, 27599 收起 <<
NCT00781430	Hepatic Insufficiency	Phase 1	Completed	-	Russian Federation ... 展开 >> Pfizer Investigational Site Moscow, Russian Federation, 125206 收起 <<
NCT03094052	HER2-positive Breast Cancer	Phase 2	Recruiting	December 2, 2020	United States, California ... 展开 >> UCSF Helen Diller Family Comprehensive Cancer Center Recruiting San Francisco, California, United States, 94115 Contact: Jo Chien 877-827-3222 cancertrials@ucsf.edu Principal Investigator: Jo Chien, MD 收起 <<
NCT02334501	Healthy	Phase 1	Completed	-	United States, Arizona ... 展开 >> Celerion Tempe, Arizona, United States, 85283 收起 <<
NCT00741260	Breast Cancer	Phase 1 Phase 2	Completed	-	-
NCT00838539	-		Completed	-	-
NCT03101748	Malignant Neoplasm of Breast	Phase 1 Phase 2	Recruiting	January 2026	United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact blim@mdanderson.org 收起 <<
NCT00741260	-		Completed	-	-
NCT00300781	-		Completed	-	-
NCT02673398	HER2 Positive Breast Carcinoma... 展开 >> Recurrent Breast Carcinoma Stage IV Breast Cancer 收起 <<	Phase 2	Recruiting	November 2018	United States, California ... 展开 >> City of Hope Corona Recruiting Corona, California, United States, 92879 Contact: Cheryl Corpus 626-256-4673 ext 81529 Sub-Investigator: Misagh Karimi, MD City of Hope Medical Center Recruiting Duarte, California, United States, 91010 Contact: Yuan Yuan, MD, PhD 800-826-4673 Principal Investigator: Yuan Yuan, MD, PhD City of Hope Antelope Valley Recruiting Lancaster, California, United States, 93534 Contact: Regan Johnson 626-256-4673 ext 25648 Sub-Investigator: Mohammad Fekrazad, MD City of Hope Mission Hills Recruiting Mission Hills, California, United States, 91345 Contact: Amy Shousha 626-256-4673 ext 81865 Sub-Investigator: Suzy Melkonian, MD City of Hope Rancho Cucamonga Recruiting Rancho Cucamonga, California, United States, 91730 Contact: Valerie Estala 626-256-4673 ext 81699 Sub-Investigator: Behnam Ebrahimi, MD City of Hope South Pasadena Recruiting South Pasadena, California, United States, 91030 Contact: Odessa Rodriguez 626-256-4673 ext 81409 Sub-Investigator: Christina Yeon, MD City of Hope West Covina Recruiting West Covina, California, United States, 91790 Contact: Mei Zheng 626-256-4673 ext 81336 Sub-Investigator: Gargi Upadhyaya, MD 收起 <<
NCT01111825	-		Completed	-	-
NCT00300781	Breast Neoplasms ... 展开 >> Neoplasms 收起 <<	Phase 2	Completed	-	-
NCT00878709	Breast Cancer	Phase 3	Active, not recruiting	November 2020	-
NCT00878709	-		Active, not recruiting	-	-
NCT01111825	Breast Cancer	Phase 1 Phase 2	Completed	-	United States, Arizona ... 展开 >> Western Regional Medical Center, Inc. Goodyear, Arizona, United States, 85338 United States, California USC/Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 United States, New York Memorial Sloan Kettering Cancer Center (MSKCC) New York, New York, United States, 10065 Weill Cornell Medical College - New York - Presbyterian Hospital New York, New York, United States, 10065 Denmark Roskilde Hospital Roskilde, Denmark, 4000 France Institut Gustave Roussy Villejuif, France, 94800 Hong Kong UNIMED Medical Institute Wan Chai, Hong Kong Spain Hospital Universitario Sant Joan de Reus Tarragona, Reus, Spain, 43204 Hospital Universitario Vall d'Hebron Barcelona, Spain, 08035 Hospital Universitari Arnau de Vilanova de Lleida Lleida, Spain, 25006 United Kingdom Edinburgh Cancer Center, Western General Hospital Edinburgh, United Kingdom, EH4 2XU The Royal Marsden NHS Foundation Trust London, United Kingdom, SW3 6JJ 收起 <<
NCT01142063	-		Completed	-	United States, Connecticut ... 展开 >> Investigational Site New Haven, Connecticut, United States, 06511 收起 <<
NCT02236000	Breast Cancer	Phase 1 Phase 2	Recruiting	July 2019	United States, Florida ... 展开 >> Cleveland Clinic Weston Recruiting Weston, Florida, United States, 33331 United States, Illinois Cancer Care Specialists of Central Illinois Recruiting Decatur, Illinois, United States, 62526 Crossroads Cancer Center Recruiting Effingham, Illinois, United States, 62401 Cancer Care Specialists of Central Illinois-Swansea Recruiting Swansea, Illinois, United States, 62226 United States, Ohio Cleveland Clinic Recruiting Cleveland, Ohio, United States, 44195 Contact: Diana Gosik, RN, BS 800-270-3165 United States, Oklahoma Stephenson Cancer Center at the University of Oklahoma Health Services Center Recruiting Oklahoma City, Oklahoma, United States, 73104 United States, Pennsylvania UPMC- Hillman Cancer Center-Monroeville Recruiting Monroeville, Pennsylvania, United States, 15146 Alleheny General Hospital Recruiting Pittsburgh, Pennsylvania, United States, 15212 Hillman Cancer Center Recruiting Pittsburgh, Pennsylvania, United States, 15213 Magee Womens Hospital of UPMC Recruiting Pittsburgh, Pennsylvania, United States, 15213 Contact: Diana Gosik, RN, BS 800-270-3165 University of Pittsburgh Recruiting Pittsburgh, Pennsylvania, United States, 15213 UPMC- St. Margaret Recruiting Pittsburgh, Pennsylvania, United States, 15215 United States, Rhode Island Women & Infants Hospital of Rhode Island Recruiting Providence, Rhode Island, United States, 02905 Contact: Diana Gosik, RN, BS 800-270-3165 United States, West Virginia West Virginia University Recruiting Morgantown, West Virginia, United States, 26501 Contact: Diana Gosik, RN, BS 800-270-3165 收起 <<
NCT01953926	Malignant Solid Tumor ... 展开 >> Fibrolamellar Carcinoma 收起 <<	Phase 2	Recruiting	March 2022	-
NCT02400476	Early Stage HER2+ Breast Cance... 展开 >>r 收起 <<	Phase 2	Recruiting	March 2020	-
NCT01960023	Colorectal Cancer	Phase 1 Phase 2	Unknown	December 2016	United States, Florida ... 展开 >> University of Florida Gainesville, Florida, United States, 32610 MD Anderson Cancer Center Orlando Orlando, Florida, United States, 32806 United States, Idaho Saint Luke's Mountain States Tumor Institute Boise, Idaho, United States, 83712 United States, Illinois Decatur Memorial Hospital Decatur, Illinois, United States, 62526 United States, Michigan Saint Joseph Mercy Hospital Ann Arbor, Michigan, United States, 48106 Henry Ford Health System Detroit, Michigan, United States, 48202 United States, North Carolina Levine Cancer Institute Charlotte, North Carolina, United States, 28204 Novant Health Presbyterian Medical Center Charlotte, North Carolina, United States, 28204 United States, Pennsylvania Thomas Jefferson University Hospital Philadelphia, Pennsylvania, United States, 19107 Allegheny General Hospital Pittsburgh, Pennsylvania, United States, 15215 University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15232 Reading Hospital and Medical Center West Reading, Pennsylvania, United States, 19611 收起 <<
NCT01827267	HER2-mutant Non-Small Cell Lun... 展开 >>g Cancer 收起 <<	Phase 2	Completed	-	United States, California ... 展开 >> City of Hope Duarte, California, United States, 91010 University of California Los Angeles Santa Monica, California, United States, 94040 United States, Colorado University of Colorado Aurora, Colorado, United States, 80045 United States, Florida Moffitt Cancer Center Tampa, Florida, United States, 33612 United States, Maryland Johns Hopkins Baltimore, Maryland, United States, 21231 United States, Massachusetts Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 Dana Farber Cancer Institute Boston, Massachusetts, United States, 02215 Massachusettes General Hospital Boston, Massachusetts, United States, 02215 United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 United States, Ohio Ohio State University Columbus, Ohio, United States, 43210 United States, Pennsylvania University of Pittsburgh Cancer Institute Pittsburgh, Pennsylvania, United States, 15232 United States, Tennessee Vanderbilt University Nashville, Tennessee, United States, 37232 United States, Texas UT Southwestern Medical Center Dallas, Texas, United States, 75390 MD Anderson Cancer Center Houston, Texas, United States, 77030 France CHU de Grenoble Hopital Albert Michallon Grenoble, France, 38043 CHRU de Lille - Hopital Calmette Lille, France, 59037 Hopital Nord Marseille, France, 13915 Hopitaux universitaires de Strasbourg Nouvel Hopital Civil Strasbourg, France, 167091 CHU de Toulous Hopital Larre Toulouse, France, 30030 Institut Gustave Roussy Villejuif, France, 94805 收起 <<
NCT00958724	Advanced Malignant Solid Tumor... 展开 >>s 收起 <<	Phase 1	Completed	-	Japan ... 展开 >> Shizuoka Cancer Center Shizuoka, Japan, 411-8777 The Cancer Institute Hospital of Japanese Foundation for Cancer Research Tokyo, Japan, 135-8550 收起 <<
NCT00958724	-		Completed	-	-
NCT01827267	-		Completed	-	-
NCT03377387	Breast Cancer	Phase 1 Phase 2	Recruiting	December 2019	United States, Connecticut ... 展开 >> Hartford Healthcare Cancer Institute @ Hartford Hospital Recruiting Hartford, Connecticut, United States, 06102 Contact: Rajani Nadkarni, MD 203-238-7747 United States, Florida Baptist Health South Florida Recruiting Miami, Florida, United States, 33143 Contact: Grace Wang, MD 305-595-2141 United States, New Jersey Memorial Sloan Kettering at Basking Ridge Recruiting Basking Ridge, New Jersey, United States, 07920 Contact: Chau Dang, MD 914-367-7181 Memorial Sloan Kettering Monmouth Recruiting Middletown, New Jersey, United States, 07748 Contact: Chau Dang, MD 914-367-7181 Memorial Sloan Kettering Bergen Recruiting Montvale, New Jersey, United States, 07645 Contact: Chau Dang, MD 914-367-7181 United States, New York Memorial Sloan Kettering Commack Recruiting Commack, New York, United States, 11725 Contact: Chau Dang, MD 914-367-7181 Memorial Sloan Kettering Westchester Recruiting Harrison, New York, United States, 10604 Contact: Chau Dang, MD 914-367-7181 Memorial Sloan Kettering Cancer Center Recruiting New York, New York, United States, 10065 Contact: Chau Dang, MD 914-367-7181 Contact: Shanu Modi, MD 646-888-4564 Principal Investigator: Chau Dang, MD Memorial Sloan Kettering Rockville Centre Recruiting Rockville Centre, New York, United States, 11570 Contact: Chau Dang, MD 914-367-7181 United States, Pennsylvania Lehigh Valley Health Network Recruiting Allentown, Pennsylvania, United States, 18103 Contact: Ranju Gupta, MD 610-402-7880 收起 <<
NCT01128842	Advanced Malignant Solid Tumor... 展开 >>s 收起 <<	Phase 1	Completed	-	Japan ... 展开 >> Investigational Site Shizuoka, Japan Investigational Site Tokyo, Japan 收起 <<
NCT03457896	Metastatic Colorectal Cancer	Phase 2	Recruiting	January 2021	United States, California ... 展开 >> Kaiser Permanente-Anaheim Recruiting Anaheim, California, United States, 92806 Kaiser Permanente-Baldwin Recruiting Baldwin Park, California, United States, 91706 Kaiser Permanente-Bellflower Recruiting Bellflower, California, United States, 90706 Kaiser Permanente-Fontana Recruiting Fontana, California, United States, 92335 Kaiser Permanente-Harbor City Recruiting Harbor City, California, United States, 90710 Kaiser Permanente-Irvine Recruiting Irvine, California, United States, 92618 Kaiser Permanente-Sunset Recruiting Los Angeles, California, United States, 90027 Kaiser Permanente-West Los Angeles (Cadillac) Recruiting Los Angeles, California, United States, 90034 Kaiser Permanente-Panorama City Recruiting Panorama City, California, United States, 91402 Kaiser Permanente-Riverside Recruiting Riverside, California, United States, 92505 Kaiser Permanente-Medical Group Recruiting San Diego, California, United States, 92108 Kaiser Permanente-Zion Recruiting San Diego, California, United States, 92120 Kaiser Permanente-San Marcos Recruiting San Marcos, California, United States, 92078 Kaiser Permanente-Woodland Hills Recruiting Woodland Hills, California, United States, 91367 United States, Florida UF Health Davis Cancer Pavilion and Shands Medical Plaza Recruiting Gainesville, Florida, United States, 32608 University of Florida Recruiting Gainesville, Florida, United States, 32610 United States, Illinois Cancer Care Specialists of Central IL-Decatur Recruiting Decatur, Illinois, United States, 62526 Decatur Memorial Hospital Recruiting Decatur, Illinois, United States, 62526 Crosslands Cancer Center Recruiting Effingham, Illinois, United States, 62401 Cancer Care Specialists of Central IL-Swansea Recruiting Swansea, Illinois, United States, 62226 United States, Michigan Trinity Health Michigan Recruiting Ann Arbor, Michigan, United States, 48106 Bronson Battle Creek Recruiting Battle Creek, Michigan, United States, 49017 St. Joseph Mercy Brighton Recruiting Brighton, Michigan, United States, 48114 St. Joseph Mercy Canton Recruiting Canton, Michigan, United States, 48188 St. Joseph Mercy Chelsea Recruiting Chelsea, Michigan, United States, 48118 Cancer Research Consortium of West Michigan Recruiting Grand Rapids, Michigan, United States, 49503-2560 Spectrum Health Butterworth Recruiting Grand Rapids, Michigan, United States, 49503 St. Mary Mercy Hospital Recruiting Livonia, Michigan, United States, 48154 Mercy Health Mercy Campus Recruiting Muskegon, Michigan, United States, 49444 St. Mary's of Michigan Recruiting Saginaw, Michigan, United States, 48601 Lakeland Healthcare-Marie Yeager Cancer Center Recruiting Saint Joseph, Michigan, United States, 49085 Metro Health Hospital Recruiting Wyoming, Michigan, United States, 49519 United States, Tennessee Wellmont Cancer Institute Recruiting Johnson City, Tennessee, United States, 37601 Wellmont Cancer Institute Recruiting Kingston, Tennessee, United States, 37660 United States, Virginia Wellmont Medical Associates-Oncology and Hematology Recruiting Bristol, Virginia, United States, 24201 Southwest Virginia Regional Cancer Center Recruiting Norton, Virginia, United States, 24273 收起 <<
NCT03065387	Malignant Neoplasm of Breast ... 展开 >> Malignant Neoplasms of Digestive Organs Malignant Neoplasms of Female Genital Organs Malignant Neoplasms of Ill-defined Secondary and Unspecified Sites Malignant Neoplasms of Independent (Primary) Multiple Sites Malignant Neoplasms of Lip Oral Cavity and Pharynx Malignant Neoplasms of Mesothelial and Soft Tissue Malignant Neoplasms of Respiratory and Intrathoracic Organs Malignant Neoplasms of Thyroid and Other Endocrine Glands Malignant Neoplasms of Urinary Tract Neoplasms of Uncertain or Unknown Behavior 收起 <<	Phase 1	Recruiting	October 2023	United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact spihapau@mdanderson.org 收起 <<
NCT03289039	Breast Cancer	Phase 2	Recruiting	March 31, 2025	United States, Indiana ... 展开 >> Indiana University Recruiting Indianapolis, Indiana, United States, 46202 Contact: Tarah Ballinger, MD Tarahb@iu.edu Principal Investigator: Tarah Ballinger, MD United States, Maine Eastern Maine Medical Center Recruiting Brewer, Maine, United States, 04412 Contact: Sarah Sinclair, MD ssinclair@emhs.org United States, Massachusetts Dana Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02115 Contact: Heather A. Parsons, MD HeatherA_Parsons@dfci.harvard.edu Principal Investigator: Heather A. Parson, MD United States, New Hampshire Dana-Farber/New Hampshire Oncology-Hematology Recruiting Londonderry, New Hampshire, United States, 03053 Contact: Fred Briccetti, MD fred_briccetti@dfci.harvard.edu Principal Investigator: Fred Briccetti, MD United States, Ohio The Ohio State University Recruiting Columbus, Ohio, United States, 43210 Contact: Robert Wesolowski, MD Robert.Wesolowski@osumc.edu United States, Texas UT Southwestern Recruiting Dallas, Texas, United States, 75390 Contact: Barbara Haley, MD barbara.haley@utsouthwestern.edu 收起 <<
NCT01808573	HER2+ Metastatic Breast Cancer... 展开 >> (MBC) 收起 <<	Phase 3	Active, not recruiting	February 2019	-
NCT02932280	Solid Tumor C... 展开 >>entral Nervous System Tumor Lymphoma Leukemia 收起 <<	Phase 1 Phase 2	Recruiting	October 2019	United States, Arizona ... 展开 >> Phoenix Children'S Hospital Recruiting Phoenix, Arizona, United States, 85016 Contact: Jessica Boklan, MD 602-546-0920 Principal Investigator: Jessica Boklan, MD United States, Arkansas Arkansas Children's Hospital Recruiting Little Rock, Arkansas, United States, 72206 Contact: Kathleen Neville, MD, MS 816-364-4405 Principal Investigator: Kathleen Neville, MD, MS United States, California Stanford University School of Medicine and Stanford Cancer Institute Recruiting Palo Alto, California, United States, 94304 Contact: Norman Lacayo, MD 650-723-5533 Principal Investigator: Norman Lacayo, MD United States, Florida Arnold Palmer Hospital for Children Recruiting Orlando, Florida, United States, 32806 Contact: Amy Smith, MD 321-841-8588 United States, New York Memorial Sloan Kettering Cancer Center Recruiting New York, New York, United States, 10065 Contact: Tanya Trippett, MD 212-639-8267 Contact: Manjusha Namuduri, MD 212-639-7937 Principal Investigator: Tanya Trippett, MD United States, Pennsylvania Pennsylvania State Hershey Children's Hospital Recruiting Hershey, Pennsylvania, United States, 17033 Contact: Valerie Brown, MD. PhD 717-531-6012 United States, Texas University of Texas Recruiting San Antonio, Texas, United States, 78229 Contact: Anne-Marie Langevin, MD 210-743-2300 Principal Investigator: Anne-Marie Langevin, MD United States, Utah Huntsman Cancer Institue Not yet recruiting Salt Lake City, Utah, United States, 84113 Contact: Luke Maese, DO 801-213-6226 Canada, Alberta Alberta Children'S Hospital Recruiting Calgary, Alberta, Canada, T3B 6A8 Contact: Aru Narendran, MD, PhD 403.210.6418 Principal Investigator: Aru Narendran, MD 收起 <<

3T3		Growth Inhibition Assay		IC50=700 ± 78 nM	15173008
3T3/neu		Growth Inhibition Assay		IC50=3 ± 0.14 nM	15173008
A431		Growth Inhibition Assay		IC50=81 ± 9 nM	15173008
A549		Growth Inhibition Assay		inhibits cell growth in time and dose dependent manner	16818618
A775insYVMA		Cell Viability Assay		decreases cell viability in time and dose dependent manner	17311002
BT 474		Growth Inhibition Assay		IC50=2 ± 0.06 nM	15173008
BT-20		Growth Inhibition Assay		IC50=0.07 μM	24009064
BT474		Growth Inhibition Assay		IC50=0.00323 ± 0.00075 μM	23816254
BT-474		Growth Inhibition Assay		IC50<0.005 μM	24009064
BT-549		Growth Inhibition Assay		IC50=1.14 μM	24009064
CAL-51		Growth Inhibition Assay		IC50=1.89 μM	24009064
CAMA-1		Growth Inhibition Assay		IC50=0.37 μM	24009064
EFM-19		Growth Inhibition Assay		IC50=0.11 μM	24009064
EFM-192A		Growth Inhibition Assay		IC50<0.005 μM	24009064
G776insV_G/C		Cell Viability Assay		decreases cell viability in time and dose dependent manner	17311002
G776insV_G/L		Cell Viability Assay		decreases cell viability in time and dose dependent manner	17311002
H3255		Growth Inhibition Assay		inhibits cell growth in time and dose dependent manner	16818618
HCC1143		Growth Inhibition Assay		IC50=0.54 μM	24009064
HCC1187		Growth Inhibition Assay		IC50=0.10 μM	24009064
HCC1395		Growth Inhibition Assay		IC50=0.49 μM	24009064
HCC1569		Growth Inhibition Assay		IC50<0.005 μM	24009064
HCC1806		Growth Inhibition Assay		IC50=0.44 μM	24009064
HCC1937		Growth Inhibition Assay		IC50=0.50 μM	24009064
HCC1954		Growth Inhibition Assay		IC50<0.005 μM	24009064
HCC38		Growth Inhibition Assay		IC50=0.25 μM	24009064
HCC70		Growth Inhibition Assay		IC50=0.03 μM	24009064
HCC827		Growth Inhibition Assay		inhibits cell growth in time and dose dependent manner	16818618
HEK293/ABCB1		Growth Inhibition Assay		IC50=6.91 ± 0.70 μM	22491935
HEK293/pcDNA3.1		Growth Inhibition Assay		IC50=5.29 ± 0.53 μM	22491935
HL60		Growth Inhibition Assay		IC50=2.26 ± 0.23 μM	22491935
HL60/Adr		Growth Inhibition Assay		IC50=1.42 ± 0.15 μM	22491935
KB		Growth Inhibition Assay		IC50=4.13 ± 0.47 μM	22491935
KBv200		Growth Inhibition Assay		IC50=6.03 ± 0.64 μM	22491935
KPL-1		Growth Inhibition Assay		IC50=1.89 μM	24009064
L858R(EGFR)		Cell Viability Assay		decreases cell viability in time and dose dependent manner	17311002
L858R/T790M(EGFR)		Cell Viability Assay		decreases cell viability in time and dose dependent manner	17311002
MCF-7		Growth Inhibition Assay		IC50=0.41 μM	24009064
MCF-7		Growth Inhibition Assay		IC50=3.30 ± 0.41 μM	22491935
MCF-7		Growth Inhibition Assay		IC50=3.02 ± 0.34 μM	22491935
MCF-7/Adr		Growth Inhibition Assay		IC50= 2.88 ± 0.30 μM	22491935
MCF-7/FLV1000		Growth Inhibition Assay		IC50=7.09 ± 0.71 μM	22491935
MDA-MB-134		Growth Inhibition Assay		IC50=0.17 μM	24009064
MDA-MB-157		Growth Inhibition Assay		IC50=1.12 μM	24009064
MDA-MB-175		Growth Inhibition Assay		IC50<0.005 μM	24009064
MDA-MB-231		Growth Inhibition Assay		IC50=1.00 μM	24009064
MDA-MB-361		Growth Inhibition Assay		IC50<0.005 μM	24009064
MDA-MB-415		Growth Inhibition Assay		IC50=0.42 μM	24009064
MDA-MB-435		Growth Inhibition Assay		IC50=0.33 μM	24009064
MDA-MB-435		Growth Inhibition Assay		IC50=960 ± 165 nM	15173008
MDA-MB-436		Growth Inhibition Assay		IC50=0.41 μM	24009064
MDAMB453		Growth Inhibition Assay		IC50=1.59 ± 0.179 μM	23816254
MDA-MB-453		Growth Inhibition Assay		IC50=0.09 μM	24009064
MDA-MB-468		Growth Inhibition Assay		IC50=0.33 μM	24009064
NCI-H1781		Growth Inhibition Assay		inhibits cell growth in time and dose dependent manner	16818618
NCI-H1975		Growth Inhibition Assay		inhibits cell growth in time and dose dependent manner	16818618
P780insGSP		Cell Viability Assay		decreases cell viability in time and dose dependent manner	17311002
SKBR	0.01-100 nM	Growth Inhibition Assay	3-7 d	inhibits cell growth in time and dose dependent manner	21487605
SKBR3		Growth Inhibition Assay		IC50=0.0075 ± 0.005 μM	23816254
SK-BR-3		Growth Inhibition Assay		IC50<0.005 μM	24009064
SK-Br-3		Growth Inhibition Assay		IC50=2 ± 0.18 nM	15173008
SUM-190		Growth Inhibition Assay		IC50=0.01 μM	24009064
SUM-225		Growth Inhibition Assay		IC50=0.01 μM	24009064
SW620		Growth Inhibition Assay		IC50=690 ± 84 nM	15173008
T-47D		Growth Inhibition Assay		IC50=0.16 μM	24009064
UACC-732		Growth Inhibition Assay		IC50=0.65 μM	24009064
UACC-812		Growth Inhibition Assay		IC50<0.005 μM	24009064
UACC-893		Growth Inhibition Assay		IC50<0.005 μM	24009064
wild-type		Cell Viability Assay		decreases cell viability in time and dose dependent manner	17311002
ZR-75-1		Growth Inhibition Assay		IC50=0.03 μM	24009064

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EGFR/ErbB1	EGFR, IC50:92 nM
HER2/ErbB2	HER2, IC50:59 nM
HER2	HER2, IC50:59 nM

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