Neratinib maleate | HKI-272 maleate | HER2/EGFR Inhibitor

Neratinib maleate {[allProObj[0].p_purity_real_show]}

货号：A165844 同义名： HKI-272 maleate

Neratinib maleate(HKI-272) 苹果酸盐是一种口服可用、不可逆且高度选择性的 HER2 和 EGFR 抑制剂，其 IC50 分别为 59 nM 和 92 nM。

Neratinib maleate 化学结构
CAS号：915942-22-2

Neratinib maleate 3D分子结构
CAS号：915942-22-2

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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/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	++++ 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 (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					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM EGFR^L858R/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。

Neratinib maleate 生物活性

描述

Neratinib (HKI-272) maleate is an orally administered, irreversible inhibitor with high selectivity for HER2 and EGFR, exhibiting IC50 values of 59 nM and 92 nM, respectively. This specificity underlines its potential therapeutic application in targeting certain cancers^[1].

体内研究

In vivo, Neratinib (administered at dosages between 0 to 80 mg/kg/day orally for 42 days) has shown to exhibit anticancer activities against cells expressing high levels of HER-2 or EGFR, further affirming its therapeutic potential^[1].

体外研究

Importantly, Neratinib shows no inhibitory activity against a range of other serine-threonine kinases and the tyrosine kinase c-Met, indicating its targeted action against HER2 and EGFR without affecting these other kinases^[1].

In cellular studies, Neratinib demonstrates a capacity to inhibit the proliferation of cell lines with high HER-2 levels, such as 3T3/neu, SK-Br-3, and BT474, while showing minimal activity in cell lines lacking HER-2 or EGFR expression. This specificity underscores its potential utility in treating cancers with elevated HER-2 or EGFR levels^[1].

Neratinib induces cell cycle arrest at the G1-S phase in BT474 cells when administered at concentrations ranging from 0 to 2 nM for 12 to 16 hours, highlighting its impact on cell proliferation dynamics^[1].

Neratinib maleate 细胞实验

Cell Line SKBR3 PANC1 cells TBCP-1 MDA-MB-453 MDA-MB-361 BT-474 SK-BR-3 HCC1954 HCC1954-N HME2-BM cells Jurkat T cells HL60 cells T cell lymphoma cells INS-1E cells Human islet cells HME2 cells Pancreatic cancer cells	Concentration	Treated Time	Description	References
SKBR3	5 nM	1 hour	To evaluate the effect of Neratinib on SKBR3 cells, results showed that Neratinib significantly inhibited HER2 signaling in SKBR3 cells.	Breast Cancer Res. 2019 Aug 13;21(1):94.
PANC1 cells	100 nM	12 hours	To evaluate the cytotoxic effect of Neratinib on PANC1 cells, results showed that Neratinib caused ~15–20% cell killing.	Oncogene. 2019 Jul;38(30):5890-5904.
TBCP-1	300 nM	24 hours	To evaluate the effect of Neratinib on TBCP-1 cells, results showed that Neratinib significantly inhibited TBCP-1 cell proliferation and induced ferroptosis.	Breast Cancer Res. 2019 Aug 13;21(1):94.
MDA-MB-453	10 nM	24 hours	Neratinib monotherapy significantly inhibited cell viability compared to control or trastuzumab, and its combination with trastuzumab was also the most potent combination.	Br J Cancer. 2024 Jun;130(12):1990-2002.
MDA-MB-361	10 nM	24 hours	Neratinib monotherapy significantly inhibited cell viability compared to control or trastuzumab, and its combination with trastuzumab was also the most potent combination.	Br J Cancer. 2024 Jun;130(12):1990-2002.
BT-474	1 µM	24 hours	To evaluate the effect of Neratinib on downstream signaling pathways. Results showed that Neratinib alone reduced phosphorylation levels of ERK1/2, Akt, and S6K.	Clin Cancer Res. 2021 Mar 15;27(6):1681-1694.
SK-BR-3	1 µM	24 hours	To evaluate the effect of Neratinib on downstream signaling pathways. Results showed that Neratinib alone reduced phosphorylation levels of ERK1/2, Akt, and S6K.	Clin Cancer Res. 2021 Mar 15;27(6):1681-1694.
HCC1954	150 nM	24 hours	To evaluate the effect of Neratinib and Dasatinib on intracellular signaling, results showed that Neratinib significantly inhibited EGFR phosphorylation	Transl Oncol. 2024 Nov;49:102073.
HCC1954-N	150 nM	24 hours	To evaluate the effect of Neratinib and Dasatinib on intracellular signaling, results showed that Neratinib significantly inhibited EGFR Y1068 phosphorylation	Transl Oncol. 2024 Nov;49:102073.
HME2-BM cells	100 nM	4 weeks	To evaluate the effect of Neratinib on the drug resistance of HME2-BM cells, results showed that HME2-BM cells were able to spontaneously develop resistance after prolonged Neratinib treatment.	Mol Biomed. 2022 Jun 22;3(1):19.
Jurkat T cells	50 nM	6 hours	To evaluate the effect of Neratinib on the expression of K-RAS, MST3, and MST4 in Jurkat T cells, results showed that Neratinib significantly reduced the expression of these proteins.	Oncogene. 2019 Jul;38(30):5890-5904.
HL60 cells	50 nM	6 hours	To evaluate the effect of Neratinib on the expression of K-RAS, MST3, and MST4 in HL60 cells, results showed that Neratinib significantly reduced the expression of these proteins.	Oncogene. 2019 Jul;38(30):5890-5904.
T cell lymphoma cells	50 nM	6 hours	Neratinib significantly reduced the total expression and phosphorylation of MST4.	J Cell Physiol. 2020 Nov;235(11):7889-7899.
INS-1E cells	5 µM, 10 µM	72 hours	Neratinib potently inhibited H2O2- and high glucose/palmitate-induced MST1 activation and apoptosis in β-cells	Nat Commun. 2019 Nov 1;10(1):5015.
Human islet cells	10 µM, 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.
HME2 cells	1 µM	96 hours	To evaluate the inhibitory effect of Neratinib on HER2 phosphorylation, results showed that Neratinib significantly inhibited HER2 phosphorylation and led to receptor degradation.	Mol Biomed. 2022 Jun 22;3(1):19.
Pancreatic cancer cells	50 nM		Neratinib exhibited lethality in pancreatic cancer cells, and its lethality was enhanced when combined with HDAC inhibitors.	J Cell Physiol. 2020 Nov;235(11):7889-7899.

Cell Line

Concentration

Treated Time

Description

References

SKBR3

5 nM

1 hour

To evaluate the effect of Neratinib on SKBR3 cells, results showed that Neratinib significantly inhibited HER2 signaling in SKBR3 cells.

Breast Cancer Res. 2019 Aug 13;21(1):94.

PANC1 cells

100 nM

12 hours

To evaluate the cytotoxic effect of Neratinib on PANC1 cells, results showed that Neratinib caused ~15–20% cell killing.

Oncogene. 2019 Jul;38(30):5890-5904.

TBCP-1

300 nM

24 hours

To evaluate the effect of Neratinib on TBCP-1 cells, results showed that Neratinib significantly inhibited TBCP-1 cell proliferation and induced ferroptosis.

Breast Cancer Res. 2019 Aug 13;21(1):94.

MDA-MB-453

10 nM

24 hours

Neratinib monotherapy significantly inhibited cell viability compared to control or trastuzumab, and its combination with trastuzumab was also the most potent combination.

Br J Cancer. 2024 Jun;130(12):1990-2002.

MDA-MB-361

10 nM

24 hours

Neratinib monotherapy significantly inhibited cell viability compared to control or trastuzumab, and its combination with trastuzumab was also the most potent combination.

Br J Cancer. 2024 Jun;130(12):1990-2002.

BT-474

1 µM

24 hours

To evaluate the effect of Neratinib on downstream signaling pathways. Results showed that Neratinib alone reduced phosphorylation levels of ERK1/2, Akt, and S6K.

Clin Cancer Res. 2021 Mar 15;27(6):1681-1694.

SK-BR-3

1 µM

24 hours

To evaluate the effect of Neratinib on downstream signaling pathways. Results showed that Neratinib alone reduced phosphorylation levels of ERK1/2, Akt, and S6K.

Clin Cancer Res. 2021 Mar 15;27(6):1681-1694.

HCC1954

150 nM

24 hours

To evaluate the effect of Neratinib and Dasatinib on intracellular signaling, results showed that Neratinib significantly inhibited EGFR phosphorylation

Transl Oncol. 2024 Nov;49:102073.

HCC1954-N

150 nM

24 hours

To evaluate the effect of Neratinib and Dasatinib on intracellular signaling, results showed that Neratinib significantly inhibited EGFR Y1068 phosphorylation

Transl Oncol. 2024 Nov;49:102073.

HME2-BM cells

100 nM

4 weeks

To evaluate the effect of Neratinib on the drug resistance of HME2-BM cells, results showed that HME2-BM cells were able to spontaneously develop resistance after prolonged Neratinib treatment.

Mol Biomed. 2022 Jun 22;3(1):19.

Jurkat T cells

50 nM

6 hours

To evaluate the effect of Neratinib on the expression of K-RAS, MST3, and MST4 in Jurkat T cells, results showed that Neratinib significantly reduced the expression of these proteins.

Oncogene. 2019 Jul;38(30):5890-5904.

HL60 cells

50 nM

6 hours

To evaluate the effect of Neratinib on the expression of K-RAS, MST3, and MST4 in HL60 cells, results showed that Neratinib significantly reduced the expression of these proteins.

Oncogene. 2019 Jul;38(30):5890-5904.

T cell lymphoma cells

50 nM

6 hours

Neratinib significantly reduced the total expression and phosphorylation of MST4.

J Cell Physiol. 2020 Nov;235(11):7889-7899.

INS-1E cells

5 µM, 10 µM

72 hours

Neratinib potently inhibited H2O2- and high glucose/palmitate-induced MST1 activation and apoptosis in β-cells

Nat Commun. 2019 Nov 1;10(1):5015.

Human islet cells

10 µM, 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.

HME2 cells

1 µM

96 hours

To evaluate the inhibitory effect of Neratinib on HER2 phosphorylation, results showed that Neratinib significantly inhibited HER2 phosphorylation and led to receptor degradation.

Mol Biomed. 2022 Jun 22;3(1):19.

Pancreatic cancer cells

50 nM

Neratinib exhibited lethality in pancreatic cancer cells, and its lethality was enhanced when combined with HDAC inhibitors.

J Cell Physiol. 2020 Nov;235(11):7889-7899.

Neratinib maleate 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 xenografts (PDXs) HER2-positive breast cancer xenograft models HER2+ breast cancer model CW2 xenograft model STZ-induced type 1 diabetes model and obese Leprdb/db diabetes model Neratinib-induced diarrhea model HER2-positive breast cancer brain metastasis model HCC1954 xenograft model	Administration	Dosage	Frequency	Description	References
Nude mice	Patient-derived xenografts (PDXs)	Oral	10 mg/kg	Daily for the duration of the experiment	To evaluate the effect of Neratinib in combination with other inhibitors on tumor growth in HER2+ PDX models. Results showed that the combination of Neratinib with palbociclib significantly reduced tumor volume and extended event-free survival in all five PDX models.	Clin Cancer Res. 2021 Mar 15;27(6):1681-1694.
Mice	HER2-positive breast cancer xenograft models	Oral	20 mg/kg	Once daily, 5 days/week	To evaluate the therapeutic benefit of N+T and compare its efficacy to P+T using HER2+breast cancer xenograft models. The results showed that N+T was more effective than P+T in accelerating tumor regression and achieving complete response.	NPJ Breast Cancer. 2021 May 27;7(1):63
NSG mice	HER2+ breast cancer model	Oral gavage	27 mg/kg	Every other day, until tumors reached 1000 mm3	To evaluate the therapeutic effect of Neratinib on HER2+ breast cancer model, results showed that Neratinib significantly inhibited the growth of HME2 parental tumors, but had a smaller effect on the growth of HME2-BM tumors, and overexpression of TG2 diminished the effectiveness of Neratinib.	Mol Biomed. 2022 Jun 22;3(1):19.
Mice	CW2 xenograft model	Oral gavage	40 mg/kg	Once daily for 14 days	To study the effect of combined neratinib and alpelisib on tumor growth in CW2 xenograft models.	Cancer Cell. 2021 Aug 9;39(8):1099-1114.e8
Mice	STZ-induced type 1 diabetes model and obese Leprdb/db diabetes model	Intraperitoneal injection	5 mg/kg	Daily for 35 days (STZ model) or 31 days (db/db model)	Neratinib significantly attenuated hyperglycemia and restored 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	50 mg/kg	Once daily for 28 days	To investigate the impact of antibiotics on neratinib-induced diarrhea. Results showed that vancomycin or neomycin significantly reduced diarrhea levels, while the broad-spectrum antibiotic cocktail was less effective.	Neoplasia. 2022 Aug;30:100806
BALB/C mice	HER2-positive breast cancer brain metastasis model	Oral gavage	60 mg/kg	Once daily for 3 weeks	To evaluate the efficacy of Neratinib in a preventive neoadjuvant setting, results showed that Neratinib significantly prolonged survival and reduced the incidence of brain metastases.	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 on, 2 days off for 10 weeks	To evaluate the anti-tumor effect of Neratinib and Dasatinib in vivo on HCC1954 xenograft model, results showed that the combination significantly inhibited tumor growth	Transl Oncol. 2024 Nov;49:102073.

Species

Nude mice Mice NSG mice Mice Mice Female Albino Wistar rats BALB/C mice BALB/c Nude mice

Animal Model

Patient-derived xenografts (PDXs) HER2-positive breast cancer xenograft models HER2+ breast cancer model CW2 xenograft model STZ-induced type 1 diabetes model and obese Leprdb/db diabetes model Neratinib-induced diarrhea model HER2-positive breast cancer brain metastasis model HCC1954 xenograft model

Administration

Dosage

Frequency

Description

References

Nude mice

Patient-derived xenografts (PDXs)

Oral

10 mg/kg

Daily for the duration of the experiment

To evaluate the effect of Neratinib in combination with other inhibitors on tumor growth in HER2+ PDX models. Results showed that the combination of Neratinib with palbociclib significantly reduced tumor volume and extended event-free survival in all five PDX models.

Clin Cancer Res. 2021 Mar 15;27(6):1681-1694.

Mice

HER2-positive breast cancer xenograft models

Oral

20 mg/kg

Once daily, 5 days/week

To evaluate the therapeutic benefit of N+T and compare its efficacy to P+T using HER2+breast cancer xenograft models. The results showed that N+T was more effective than P+T in accelerating tumor regression and achieving complete response.

NPJ Breast Cancer. 2021 May 27;7(1):63

NSG mice

HER2+ breast cancer model

Oral gavage

27 mg/kg

Every other day, until tumors reached 1000 mm3

To evaluate the therapeutic effect of Neratinib on HER2+ breast cancer model, results showed that Neratinib significantly inhibited the growth of HME2 parental tumors, but had a smaller effect on the growth of HME2-BM tumors, and overexpression of TG2 diminished the effectiveness of Neratinib.

Mol Biomed. 2022 Jun 22;3(1):19.

Mice

CW2 xenograft model

Oral gavage

40 mg/kg

Once daily for 14 days

To study the effect of combined neratinib and alpelisib on tumor growth in CW2 xenograft models.

Cancer Cell. 2021 Aug 9;39(8):1099-1114.e8

Mice

STZ-induced type 1 diabetes model and obese Leprdb/db diabetes model

Intraperitoneal injection

5 mg/kg

Daily for 35 days (STZ model) or 31 days (db/db model)

Neratinib significantly attenuated hyperglycemia and restored 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

50 mg/kg

Once daily for 28 days

To investigate the impact of antibiotics on neratinib-induced diarrhea. Results showed that vancomycin or neomycin significantly reduced diarrhea levels, while the broad-spectrum antibiotic cocktail was less effective.

Neoplasia. 2022 Aug;30:100806

BALB/C mice

HER2-positive breast cancer brain metastasis model

Oral gavage

60 mg/kg

Once daily for 3 weeks

To evaluate the efficacy of Neratinib in a preventive neoadjuvant setting, results showed that Neratinib significantly prolonged survival and reduced the incidence of brain metastases.

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 on, 2 days off for 10 weeks

To evaluate the anti-tumor effect of Neratinib and Dasatinib in vivo on HCC1954 xenograft model, results showed that the combination significantly inhibited tumor growth

Transl Oncol. 2024 Nov;49:102073.

Neratinib maleate 参考文献

Neratinib maleate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.49mL

0.30mL

0.15mL

7.43mL

1.49mL

0.74mL

14.86mL

2.97mL

1.49mL

Neratinib maleate 技术信息

CAS号	915942-22-2
分子式	C₃₄H₃₃ClN₆O₇
分子量	673.11
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.O=C(O)/C=C\C(O)=O
MDL No.	MFCD30607264

别名	HKI-272 maleate
运输	蓝冰
InChI Key	VXZCUHNJXSIJIM-MEBGWEOYSA-N
Pubchem ID	67307512

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 250 mg/mL(371.41 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

Neratinib maleate {[allProObj[0].p_purity_real_show]}

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