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/ Lapatinib ditosylate/二甲苯磺酸拉帕替尼

Lapatinib ditosylate/二甲苯磺酸拉帕替尼 {[allProObj[0].p_purity_real_show]}

货号：A208985 同义名： 二对甲苯磺酸拉帕替尼 / GW572016 ditosylate; GW2016 ditosylate

Lapatinib ditosylate (GW572016 ditosylate) 是一种强效的ErbB-2和EGFR酪氨酸激酶结构域抑制剂，对纯化EGFR和ErbB-2的IC50值分别为10.2 nM和9.8 nM。

Lapatinib ditosylate/二甲苯磺酸拉帕替尼 化学结构 CAS号：388082-77-7
Lapatinib ditosylate/二甲苯磺酸拉帕替尼 化学结构
CAS号：388082-77-7
Lapatinib ditosylate/二甲苯磺酸拉帕替尼 3D分子结构
CAS号：388082-77-7
Lapatinib ditosylate/二甲苯磺酸拉帕替尼 化学结构 CAS号：388082-77-7
Lapatinib ditosylate/二甲苯磺酸拉帕替尼 3D分子结构 CAS号：388082-77-7
规格 价格 会员价 库存 数量
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Lapatinib ditosylate/二甲苯磺酸拉帕替尼 纯度/质量文件 产品仅供科研

货号：A208985 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
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产品名称 EGFR/ErbB1 ↓ ErbB3 ↓ ErbB4 ↓ HER2/ErbB2 ↓ mutant EGFR ↓ 其他靶点 纯度
WZ-3146 ++++

EGFR (E746_A750/T790M), IC50: 14 nM

EGFR (E746_A750), IC50: 2 nM

 		99%+
Daphnetin +

EGFR, IC50: 7.67 μM

 		PKA,PKC 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 (L858R), IC50: 0.2 nM

EGFR (WT), IC50: 0.3 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), IC50: 2 nM

EGFR (L858R/T790M), IC50: 8 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 (L858R), IC50: 6 nM

EGFR (L861Q) , IC50: <1 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 L858R, IC50: 2 nM

EGFR(d746-750), IC50: 1.4 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

 		++++

EGFRL858R/T790M, IC50: 0.51 nM

EGFRT790M, 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 (L858R), IC50: 10 nM

EGFR (wt), IC50: 0.5 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(del19), IC50: 39.9 nM

EGFR(C797S/T790M/del19), IC50: 67.2 nM

 		ALK,FLT3 98%
Avitinib ++++

EGFR L858R/T790M, IC50: 0.18 nM

 		BTK 99%+
EAI045 ✔ 97%
Almonertinib ✔ 99%
BI-4020 ++++

EGFRdel19 T790M C797S, IC50: 0.2 nM

 		99%+
EGFR-IN-7 ++++

EGFRd746-750/T790M/C797S, IC50: 0.26 nM

EGFRL858R/T790M, IC50: 0.19 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。

Lapatinib ditosylate/二甲苯磺酸拉帕替尼 生物活性

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. Lapatinib Ditosylate is the ditosylate form of lapatinib. Lapatinib is a potent and selective inhibitor of ErbB-2 and EGFR with IC50 values of 9.8nM and 10.2nM (measured by kinase activity assay), respectively. Treatment with lapatinib at concentration ranging in 0.03-10μM for 6h caused dose-dependent decrease of autophosphorylation of both EGFR and ErbB-2 in HN5 and BT474 cells, alone with the decreased phosphorylation level of the key signal transduction mediator AKT. Cell lines with overexpression of ErbB-2 or EGFR, including A431, HN5, BT474, N87, CaLu-3 and HB4a c5.2, were more sensitive to lapatinib with IC50 values ranging in 0.09-0.21μM 72h growth inhibition assays, showing the selective inhibition of cell growth by lapatinib. Induction of G1 arrest can be observed in HN5, EGFR-overexpressing cell line, treated with 1 or 10μM lapatinib. Apoptosis can be significantly induced by 10μM lapatinib after 72h in BT474 cells. Oral administration of lapatinib at dose of 100mg/kg twice daily for 21 days achieved a complete inhibition of tumor growth in both BT474 and HN5 human tumor xenografts[1].
作用机制 Lapatinib is an ATP-competitive inhibitor of both EGFR and HER2.[1]

Lapatinib ditosylate/二甲苯磺酸拉帕替尼 细胞实验

Cell Line
Concentration Treated Time Description References
BT474 cells 1 μM 18 h Inhibited HER2 phosphorylation, leading to FASN dephosphorylation Breast Cancer Res. 2010;12(6):R96.
SKBR3 cells 1 μM 18 h Inhibited HER2 phosphorylation, leading to FASN dephosphorylation Breast Cancer Res. 2010;12(6):R96.
SKBR3 cells 10 nM 72 h To evaluate the effects of dual HER2 blockade in HER2-E breast cancer cell lines, results showed dual HER2 blockade led to a significant relative increase in Luminal A and normal-like signature scores, and a relative decrease in proliferation, HER2-E, Luminal B and Basal-like signature scores Nat Commun. 2020 Jan 20;11(1):385.
BT474 cells 10 nM 72 h To evaluate the effects of dual HER2 blockade in HER2-E breast cancer cell lines, results showed dual HER2 blockade led to a significant relative increase in Luminal A and normal-like signature scores, and a relative decrease in proliferation, HER2-E, Luminal B and Basal-like signature scores Nat Commun. 2020 Jan 20;11(1):385.
UACC893 cells 1 μM 72 h To evaluate the antiproliferative effect of lapatinib on HER2+ breast cancer cells. Results showed that lapatinib inhibited HER2 phosphorylation, but the inhibitory effect on the PI3K signaling pathway was attenuated in PIK3CA mutant cells. Breast Cancer Res. 2014 Jan 23;16(1):R9.
HCC1954 cells 1 μM 72 h To evaluate the antiproliferative effect of lapatinib on HER2+ breast cancer cells. Results showed that lapatinib inhibited HER2 phosphorylation, but the inhibitory effect on the PI3K signaling pathway was attenuated in PIK3CA mutant cells. Breast Cancer Res. 2014 Jan 23;16(1):R9.
MDA-MB-361 cells 1 μM 72 h To evaluate the antiproliferative effect of lapatinib on HER2+ breast cancer cells. Results showed that lapatinib inhibited HER2 phosphorylation, but the inhibitory effect on the PI3K signaling pathway was attenuated in PIK3CA mutant cells. Breast Cancer Res. 2014 Jan 23;16(1):R9.
SKBR3 cells 1 μM 72 h To evaluate the antiproliferative effect of lapatinib on HER2+ breast cancer cells. Results showed that lapatinib inhibited HER2 phosphorylation, but the inhibitory effect on the PI3K signaling pathway was attenuated in PIK3CA mutant cells. Breast Cancer Res. 2014 Jan 23;16(1):R9.
BT474 cells 1 μM 72 h To evaluate the antiproliferative effect of lapatinib on HER2+ breast cancer cells. Results showed that lapatinib inhibited HER2 phosphorylation, but the inhibitory effect on the PI3K signaling pathway was attenuated in PIK3CA mutant cells. Breast Cancer Res. 2014 Jan 23;16(1):R9.
T47D cells 0.1 μg/mL 24 h To evaluate the inhibitory effect of Lapatinib alone or in combination with other drugs on cell proliferation. The results showed that Lapatinib alone had a significant inhibitory effect on T47D cells, but the combination with JPH203 was more effective Bioact Mater. 2021 Jul 14;9:15-28.
MCF7 cells 0.1 μg/mL 24 h To evaluate the inhibitory effect of Lapatinib alone or in combination with other drugs on cell proliferation. The results showed that Lapatinib alone had a significant inhibitory effect on MCF7 cells, but the combination with JPH203 was more effective. Bioact Mater. 2021 Jul 14;9:15-28.
A375 melanoma cells 200nM 24 h To evaluate the inhibitory effect of Lapatinib alone or in combination with Phenformin on cell proliferation. The results showed that Lapatinib alone had a significant inhibitory effect on A375 cells, but the combination with Phenformin was more effective Cell Metab. 2018 Dec 4;28(6):817-832.e8.
NT2197 cells 600 nM 24 h To evaluate the inhibitory effect of Lapatinib alone or in combination with Phenformin on cell proliferation. The results showed that Lapatinib alone had a significant inhibitory effect on NT2197 cells, but the combination with Phenformin was more effective Cell Metab. 2018 Dec 4;28(6):817-832.e8.
NUGC-4 cell lines 69 nM(GI50) 3 days Evaluate the anti-proliferative effect of Lapatinib on HER2-high gastric cancer cell lines, results showed NUGC-4 was sensitive to Lapatinib Br J Cancer. 2014 Mar 4;110(5):1169-78.
NCI-N87 cell lines 16 nM(GI50) 3 days Evaluate the anti-proliferative effect of Lapatinib on HER2-high gastric cancer cell lines, results showed NCI-N87 was sensitive to Lapatinib Br J Cancer. 2014 Mar 4;110(5):1169-78.
SkBr3 1µM 48 h To evaluate the effect of lapatinib on apoptosis in HER2-amplified breast cancer cells. BIM knockdown significantly reduced lapatinib-induced apoptosis. Cancer Discov. 2011 Sep;1(4):352-65.
EFM-192A 1µM 72 h To evaluate the effect of lapatinib on apoptosis in HER2-amplified breast cancer cells. EFM-192A cells had a lower apoptotic response (<5%). Cancer Discov. 2011 Sep;1(4):352-65.
BT-474 1µM 72 h To evaluate the effect of lapatinib on apoptosis in HER2-amplified breast cancer cells. BT-474 cells showed a more pronounced apoptotic response (~65%), while EFM-192A cells had a lower apoptotic response (<5%). Cancer Discov. 2011 Sep;1(4):352-65.
CD24HiCD49fHiLin− TIC-enriched cells 1 μM Reduced sphere-forming ability Cancer Res. 2014 Jan 1;74(1):341-52.
CD24HiCD49fHiLin− TIC-enriched cells 5 μM 10 min Inhibited Nrg1-mediated phosphorylation of Akt and Erk1/2 Cancer Res. 2014 Jan 1;74(1):341-52.

Lapatinib ditosylate/二甲苯磺酸拉帕替尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Female athymic nude mice HER2+ breast cancer xenograft model Lapatinib and BKM120: oral gavage; Trastuzumab: intraperitoneal injection 100 mg/kg Lapatinib and BKM120: once daily; Trastuzumab: twice weekly; Duration: 28 days To evaluate the antitumor effect of lapatinib combined with trastuzumab and BKM120 on HER2+ breast cancer xenograft models. Results showed that triple therapy induced tumor regression in both PIK3CA wild-type and mutant tumors, with superior efficacy compared to dual therapy. Breast Cancer Res. 2014 Jan 23;16(1):R9.
NOD/scid/Il2 γ-null (NSG) mice Human breast cancer xenograft model Oral gavage 100 mg/kg 5 days/week until tumor regression To evaluate the effect of lapatinib combined with other anti-HER2 therapies on tumor regression, results showed that combination therapy led to rapid tumor regression to a non-palpable state. Breast Cancer Res. 2021 Jun 4;23(1):63
Nude mice NT2197 xenograft model Intraperitoneal injection and gavage 50mg/kg Every 24 hours for 8 days Evaluate the anti-tumor effects of Lapatinib and phenformin combination Cell Metab. 2018 Dec 4;28(6):817-832.e8.
NOD/SCID mice HER2-positive breast cancer model Oral 100 mg/kg Once daily for 3 weeks To study the anti-tumor effect of Lapatinib and BYL719 combination therapy in HER2-positive breast cancer models. Results showed that combination therapy significantly inhibited tumor growth. Clin Transl Med. 2021 Nov;11(11):e589
Nude mice SGC031 PDGCX model Oral 100 mg/kg Twice daily for 3 weeks Evaluate the anti-tumor effect of Lapatinib in a MET-amplified and overexpressed PDGCX model, results showed Lapatinib did not significantly inhibit tumor growth Br J Cancer. 2014 Mar 4;110(5):1169-78.
NOD SCID mice HT-29 colorectal tumor xenograft model Oral gavage 60 mg/kg Once daily for 10 days To study the utility of serum phospho-CSE1L levels in early detection of targeted therapy efficacy, showing a decline in serum phospho-CSE1L levels 3 days post-treatment. J Transl Med. 2015 Jun 13;13:191.
Nude mice HER2-amplified breast cancer xenograft model Oral gavage 100mg/kg Once daily for approximately 30 days To evaluate the anti-tumor effect of lapatinib in HER2-amplified breast cancer xenograft models. High BIM-expressing BT-474 cells were more sensitive to lapatinib, while low BIM-expressing ZR7530 cells showed weaker responses. Cancer Discov. 2011 Sep;1(4):352-65.
Mice MMTV-Wnt-1 mammary tumor model Oral gavage 100 mg/kg Twice daily for 14 days Reduced CD24HiCD49fHi TIC-enriched subpopulation and inhibited tumor growth Cancer Res. 2014 Jan 1;74(1):341-52.

Lapatinib ditosylate/二甲苯磺酸拉帕替尼 动物研究

Dose Mice[2]: 2 mg/kg - 100 mg/kg (p.o.), 10 mg/kg (i.v.), rat[2]: 2 mg/kg - 10 mg/kg (p.o.), 10 mg/kg (i.v.)
Administration p.o., i.v.
Pharmacokinetics
Animal Mice[2] Rats[2] Dogs[2]
Dose 10 mg/kg 10 mg/kg 10 mg/kg
Administration i.v. i.v. i.v.
AUC∞ 3469 ng·h/ml 3596 ± 924 ng·h/ml 14087 ± 3094 ng·h/ml
T1/2 5.69 h 12.3 ± 8.24 h 5.85 ± 0.17 h
Tmax 0.5 h 0.08 h 0.08 h
CL 48.0 ml/min/kg 48.8 ± 14.3 ml/min/kg 12.2 ± 2.83 ml/min/kg
Cmax 942 ng/ml 4557 ± 1210 ng/ml 3793 ± 167 ng/ml
Vss 9.55 L/kg 6.16 ± 1.95 L/kg 5.70 ± 1.03 L/kg

Lapatinib ditosylate/二甲苯磺酸拉帕替尼 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
NCT00849329 Neoplasms, Breast Phase 1 Completed - United States, South Carolina ... 展开 >> GSK Investigational Site Greenville, South Carolina, United States, 29605 Korea, Republic of GSK Investigational Site Seoul, Korea, Republic of, 135-710 GSK Investigational Site Songpa-gu, Seoul, Korea, Republic of, 138-736 Spain GSK Investigational Site Hospitalet de Llobregat (Barcelona), Spain, 08907 收起 <<
NCT00486954 Neoplasms, Gastrointestinal Tr... 展开 >>act 收起 << Phase 3 Completed - China, Guangdong ... 展开 >> GSK Investigational Site Guangzhou, Guangdong, China, 510060 China GSK Investigational Site Beijing, China, 100021 GSK Investigational Site Beijing, China, 100071 GSK Investigational Site Shanghai, China, 200032 Japan GSK Investigational Site Tokyo, Japan, 113-8677 Korea, Republic of GSK Investigational Site Hwasun, Korea, Republic of, 519-809 GSK Investigational Site Seongnam-si Gyeonggi-do, Korea, Republic of, 463-707 GSK Investigational Site Seoul, Korea, Republic of, 110-744 GSK Investigational Site Seoul, Korea, Republic of, 120-752 GSK Investigational Site Seoul, Korea, Republic of, 135-710 Taiwan GSK Investigational Site Kaohsiung, Taiwan, 807 GSK Investigational Site Niaosong Township, Kaohsiung, Taiwan, 833 GSK Investigational Site Tainan County, Taiwan, 736 GSK Investigational Site Tainan, Taiwan, 704 GSK Investigational Site Taipei, Taiwan, 100 GSK Investigational Site Taipei, Taiwan, 112 GSK Investigational Site Tau-Yuan County, Taiwan, 333 收起 <<
NCT00486954 - Completed - -

Lapatinib ditosylate/二甲苯磺酸拉帕替尼 参考文献

[1]Pharmacokinetics of lapatinib

Lapatinib ditosylate/二甲苯磺酸拉帕替尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.08mL

0.22mL

0.11mL

5.40mL

1.08mL

0.54mL

10.81mL

2.16mL

1.08mL

Lapatinib ditosylate/二甲苯磺酸拉帕替尼 技术信息

CAS号388082-77-7
分子式C43H42ClFN4O10S3
分子量 925.46
SMILES Code O=S(CCNCC1=CC=C(C2=CC3=C(NC4=CC=C(OCC5=CC=CC(F)=C5)C(Cl)=C4)N=CN=C3C=C2)O1)(C)=O.O=S(C6=CC=C(C)C=C6)(O)=O.O=S(C7=CC=C(C)C=C7)(O)=O
MDL No. MFCD09264195
别名 二对甲苯磺酸拉帕替尼 ;GW572016 ditosylate; GW2016 ditosylate
运输蓝冰
InChI Key UWYXLGUQQFPJRI-UHFFFAOYSA-N
Pubchem ID 9941095
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 120 mg/mL(129.67 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

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

Tags: Lapatinib ditosylate | GW572016 ditosylate;GW2016 ditosylate | 二对甲苯磺酸拉帕替尼 | EGFR | HER2 | AmBeed-信号通路专用抑制剂 | Lapatinib ditosylate/二甲苯磺酸拉帕替尼 纯度/质量文件 | Lapatinib ditosylate/二甲苯磺酸拉帕替尼 亚型比较 | Lapatinib ditosylate/二甲苯磺酸拉帕替尼 生物活性 | Lapatinib ditosylate/二甲苯磺酸拉帕替尼 动物研究 | Lapatinib ditosylate/二甲苯磺酸拉帕替尼 临床数据 | Lapatinib ditosylate/二甲苯磺酸拉帕替尼 参考文献 | Lapatinib ditosylate/二甲苯磺酸拉帕替尼 实验方案 | Lapatinib ditosylate/二甲苯磺酸拉帕替尼 技术信息

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