Afatinib dimaleate | 马来酸阿法替尼 | BIBW 2992MA2 | EGFR/HER2 Inhibitor

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Afatinib dimaleate/双马来酸盐阿法替尼 {[allProObj[0].p_purity_real_show]}

货号：A170920 同义名： 马来酸阿法替尼 / BIBW 2992MA2; Afatinib (maleate)

Afatinib dimaleate（BIBW 2992）二马来酸盐是一种口服活性、高效且不可逆的ErbB家族（EGFR和HER2）双特异性抑制剂，对EGFRwt、EGFRL858R、EGFRL858R/T790M和HER2的IC50分别为0.5 nM、0.4 nM、10 nM和14 nM。它用于食管鳞状细胞癌（ESCC）、非小细胞肺癌（NSCLC）和胃癌的研究。

Afatinib dimaleate/双马来酸盐阿法替尼化学结构
CAS号：850140-73-7

Afatinib dimaleate/双马来酸盐阿法替尼 3D分子结构
CAS号：850140-73-7

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Afatinib dimaleate/双马来酸盐阿法替尼纯度/质量文件产品仅供科研

货号：A170920 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。

Afatinib dimaleate/双马来酸盐阿法替尼生物活性

靶点

EGFR/ErbB1

EGFR (wt), IC50:0.5 nM

EGFR (L858R/T790M), IC50:0.4 nM
HER2/ErbB2

HER2, IC50:14 nM
HER2

HER2, IC50:14 nM

描述

EGFR (epidermal growth factor receptor) family consists of four members that belong to the ErbB lineage of proteins (ErbB1–4) with an external domain that binds activating ligands, such as EGF, and is overexpressed in a significant percentage of carcinomas and contributes to the malignant phenotype. Upon activation, EGFR phosphorylates both the receptor itself and a variety of “effector” protein. Afatinib Dimaleate is the dimaleate form of Afatinib. Afatinib is an irreversible inhibitor of pan-ErbB inhibitor with IC50 values of 0.4nM, 0.5nM, 10nM, 14nM and 1nM for EGFR (L858R), EGFR (wt), EGFR (L858R/T790M), HER2 (measured by cell-free in vitro kinase assays) and ErbB4, respectively. Afatinib displays potent cellular effects on both EGFR and HER2 phosphorylation in cell lines with the in vitro kinase results, as well as anchorage-independent proliferation in NIH-3T3 cells ectopically expressing EGFR mutants. Afatinib inhibited survival of human NSCLC cell lines expressing HER2 776insV (NCI-H1781) or EGFR E746_A750del (HCC827), but showed no activity toward A549 cells, which expressed wild-type EGFR and HER2, but simultaneously harboring an oncogenic Kras G12S point mutation. Daily oral treatment with Afatinib at dose of 20mg/kg for 25 days resulted in dramatic tumor regression and downregulation of EGFR and AKT phosphorylation in A431 cells xenografted models. Also the tumor regression by Afatinib can be observed in NCI-N87 cells and H1975 cells xenografted animals.

Afatinib dimaleate/双马来酸盐阿法替尼细胞实验

Cell Line ICC11 cell line ICC10-6 cell line ICC21 cell line ICC13-7 cell line Hs746T cell line MKN7 cell line MKN1 cell line NCI-N87 cell line Human ESCC cell lines TE-10 Human ESCC cell lines TE-1 cell line Human ESCC cell lines KYSE510 Human ESCC cell lines KYSE140 Human ESCC cell lines KYSE450 Human ESCC cell lines EC109 ESTDAB105 ESTDAB102 SkMel2 cells A375VR4 cells A375 melanoma cells H2073-ASV cell lines H2073-SVD cell lines NCI-H1781 NCI-H2170 NSCLC cell lines Calu3 TNBC cell lines BT20 TNBC cell lines HDQP1 TNBC cell lines HCC1937	Concentration	Treated Time	Description	References
ICC11 cell line	100 nM	5 days	To evaluate the effect of Afatinib in combination with FGFR inhibitors on cell death induction in FGFR2 fusion-positive ICC cell lines. Results showed that Afatinib significantly enhanced the cell death induction effect of FGFR inhibitors.	Cancer Discov. 2022 May 2;12(5):1378-1395.
ICC10-6 cell line	100 nM	5 days	To evaluate the effect of Afatinib in combination with FGFR inhibitors on cell death induction in FGFR2 fusion-positive ICC cell lines. Results showed that Afatinib significantly enhanced the cell death induction effect of FGFR inhibitors.	Cancer Discov. 2022 May 2;12(5):1378-1395.
ICC21 cell line	100 nM	5 days	To evaluate the effect of Afatinib in combination with FGFR inhibitors on cell death induction in FGFR2 fusion-positive ICC cell lines. Results showed that Afatinib significantly enhanced the cell death induction effect of FGFR inhibitors.	Cancer Discov. 2022 May 2;12(5):1378-1395.
ICC13-7 cell line	100 nM	5 days	To evaluate the effect of Afatinib in combination with FGFR inhibitors on cell death induction in FGFR2 fusion-positive ICC cell lines. Results showed that Afatinib significantly enhanced the cell death induction effect of FGFR inhibitors.	Cancer Discov. 2022 May 2;12(5):1378-1395.
Hs746T cell line	0.001, 0.01, 0.5, or 1 μM	20 min	Hs746T cells did not respond to afatinib, and MET amplification was identified as a potential resistance factor.	Mol Oncol. 2018 Apr;12(4):441-462.
MKN7 cell line	0.001, 0.01, 0.5, or 1 μM	20 min	Trastuzumab treatment resulted in a moderate, nonsignificant decrease in HER2 phosphorylation. Afatinib slightly decreased the phosphorylation of EGFR and HER2 (nonsignificantly).	Mol Oncol. 2018 Apr;12(4):441-462.
MKN1 cell line	0.001, 0.01, 0.5, or 1 μM	20 min	Trastuzumab treatment had no effect in the cell line MKN1. Phosphorylation of EGFR was increased by EGF treatment and decreased by afatinib treatment (nonsignificantly).	Mol Oncol. 2018 Apr;12(4):441-462.
NCI-N87 cell line	0.001, 0.01, 0.5, or 1 μM	20 min	Afatinib alone or in combination with trastuzumab influenced HER kinases in all cell lines; that is, the effects of monotherapy and combination therapy were transduced to the intracellular kinase network.	Mol Oncol. 2018 Apr;12(4):441-462.
Human ESCC cell lines TE-10	0, 10 nM, 100 nM, 1 μM	48 h	To evaluate the anti-proliferative activity of Afatinib on TE-10 cells and its effects on EGFR downstream signaling molecules. Results showed that Afatinib effectively inhibited EGFR phosphorylation.	J Hematol Oncol. 2018 Aug 29;11(1):109.
Human ESCC cell lines TE-1 cell line	0, 10 nM, 100 nM, 1 μM	48 h	To evaluate the anti-proliferative activity of Afatinib on TE-1 cells and its effects on EGFR downstream signaling molecules. Results showed that Afatinib effectively inhibited EGFR phosphorylation but failed to significantly suppress pERK in insensitive cells.	J Hematol Oncol. 2018 Aug 29;11(1):109.
Human ESCC cell lines KYSE510	0, 10 nM, 100 nM, 1 μM	48 h	To evaluate the anti-proliferative activity of Afatinib on KYSE510 cells and its effects on EGFR downstream signaling molecules. Results showed that Afatinib effectively inhibited EGFR phosphorylation but failed to significantly suppress pS6 and pERK in insensitive cells.	J Hematol Oncol. 2018 Aug 29;11(1):109.
Human ESCC cell lines KYSE140	0, 10 nM, 100 nM, 1 μM	48 h	To evaluate the anti-proliferative activity of Afatinib on KYSE140 cells and its effects on EGFR downstream signaling molecules. Results showed that Afatinib effectively inhibited EGFR phosphorylation and significantly suppressed pS6 and pERK in sensitive cells.	J Hematol Oncol. 2018 Aug 29;11(1):109.
Human ESCC cell lines KYSE450	0, 10 nM, 100 nM, 1 μM	48 h	To evaluate the anti-proliferative activity of Afatinib on KYSE450 cells and its effects on EGFR downstream signaling molecules. Results showed that Afatinib effectively inhibited EGFR phosphorylation and significantly suppressed pS6 and pERK in sensitive cells.	J Hematol Oncol. 2018 Aug 29;11(1):109.
Human ESCC cell lines EC109	0, 10 nM, 100 nM, 1 μM	48 h	To evaluate the anti-proliferative activity of Afatinib on EC109 cells and its effects on EGFR downstream signaling molecules. Results showed that Afatinib effectively inhibited EGFR phosphorylation and significantly suppressed pS6 and pERK in sensitive cells.	J Hematol Oncol. 2018 Aug 29;11(1):109.
ESTDAB105	2 µM	72 h	Evaluate the effect of combination therapy on BRAF/NRAS wild-type melanoma cells, results showed significant reduction in cell viability.	Cell Death Dis. 2019 Sep 10;10(9):663.
ESTDAB102	2 µM	72 h	Evaluate the effect of combination therapy on NRAS-mutant melanoma cells, results showed significant reduction in cell viability.	Cell Death Dis. 2019 Sep 10;10(9):663.
SkMel2 cells	2 µM	72 h	Evaluate the effect of combination therapy on NRAS-mutant melanoma cells, results showed significant reduction in cell viability.	Cell Death Dis. 2019 Sep 10;10(9):663.
A375VR4 cells	2 µM	72 h	Evaluate the effect of combination therapy on drug-resistant melanoma cells, results showed significant reduction in cell viability.	Cell Death Dis. 2019 Sep 10;10(9):663.
A375 melanoma cells	2 µM	72 h	Evaluate the effect of Afatinib and Crizotinib combination therapy on melanoma cell viability, results showed significant reduction in cell viability.	Cell Death Dis. 2019 Sep 10;10(9):663.
H2073-ASV cell lines	10 nM	2 weeks	Evaluate the growth inhibitory effect of afatinib on EGFR Ex20Ins mutant cells	Mol Cancer Ther. 2018 May;17(5):885-896.
H2073-SVD cell lines	10 nM	2 weeks	Evaluate the growth inhibitory effect of afatinib on EGFR Ex20Ins mutant cells	Mol Cancer Ther. 2018 May;17(5):885-896.
NCI-H1781	5 nM-0.4 μM	6 months	Establish afatinib-resistant cell lines to study resistance mechanisms	Cancer Sci. 2018 May;109(5):1493-1502.
NCI-H2170	5 nM-2 μM	6 months	Establish afatinib-resistant cell lines to study resistance mechanisms	Cancer Sci. 2018 May;109(5):1493-1502.
NSCLC cell lines Calu3	5 nM-2 μM	6 months	Establish afatinib-resistant cell lines to study resistance mechanisms	Cancer Sci. 2018 May;109(5):1493-1502.
TNBC cell lines BT20	4.66 ± 0.32 µM(IC50）	5 days	To evaluate the antiproliferative effects of afatinib on TNBC cell lines, BT20 showed an IC50 value of 4.66 ± 0.32 µM for afatinib.	Ther Adv Med Oncol. 2020 Jan 28;12:1758835919897546.
TNBC cell lines HDQP1	0.04 ± 0.01 µM(IC50）	5 days	To evaluate the antiproliferative effects of afatinib on TNBC cell lines, HDQP1 showed an IC50 value of 0.04 ± 0.01 µM for afatinib.	Ther Adv Med Oncol. 2020 Jan 28;12:1758835919897546.
TNBC cell lines HCC1937	0.90 ± 0.28 µM(IC50）	5 days	To evaluate the antiproliferative effects of afatinib on TNBC cell lines, HCC1937 showed an IC50 value of 0.90 ± 0.28 µM for afatinib.	Ther Adv Med Oncol. 2020 Jan 28;12:1758835919897546.

Afatinib dimaleate/双马来酸盐阿法替尼动物实验

Species Mice NOD/SCID mice Mice SCID mice Mice BALB/c-nu/nu female mice Nude mice CB17/lcr-PrkdcSCID/Crl mice NSG mice	Animal Model ICC21 subcutaneous xenograft model ESCC PDX models Xenograft model H2073-SVD and H2073-ASV xenograft models WT C57BL/6J mice Calu3-ARS xenograft model Non-small cell lung cancer patient-derived xenograft (PDX) models HCC1806 xenograft model SUIT2 orthotopic model	Administration	Dosage	Frequency	Description	References
Mice	ICC21 subcutaneous xenograft model	Oral gavage	15 mg/kg	Daily for 21 days	To evaluate the in vivo efficacy of Afatinib in combination with FGFR inhibitors in FGFR2 fusion-positive ICC models. Results showed that combination treatment significantly induced tumor regression.	Cancer Discov. 2022 May 2;12(5):1378-1395.
NOD/SCID mice	ESCC PDX models	Oral gavage	15 mg/kg	Once daily for 21 days	To evaluate the anti-tumor effects of Afatinib in ESCC PDX models. Results showed that Afatinib significantly inhibited tumor growth, with TGI ranging from 82.65% to 118.4%.	J Hematol Oncol. 2018 Aug 29;11(1):109.
Mice	Xenograft model	Oral	20 mg/kg	Daily for 14 days	Evaluate the effect of combination therapy on melanoma xenograft model, results showed significant reduction in tumor growth rate.	Cell Death Dis. 2019 Sep 10;10(9):663.
SCID mice	H2073-SVD and H2073-ASV xenograft models	Oral gavage	7.5 or 20 mg/kg	Once daily for 14 days	Evaluate the tumor growth inhibitory effect of afatinib on EGFR Ex20Ins mutant tumors, results showed afatinib at 7.5 mg/kg was ineffective in H2073-SVD and H2073-ASV models	Mol Cancer Ther. 2018 May;17(5):885-896.
Mice	WT C57BL/6J mice	Oral gavage	25 mg/kg	For 2 weeks	To study the effects of ErbB signaling inhibition on VEGF-B–induced cardiac hypertrophy, results showed that afatinib inhibited VEGF-B–induced phosphorylation of Akt and Erk.	Circulation. 2019 May 28;139(22):2570-2584.
BALB/c-nu/nu female mice	Calu3-ARS xenograft model	Oral	20 mg/kg	6 days per week for 3 weeks	Evaluate the efficacy of combined afatinib and crizotinib treatment on afatinib-resistant tumors with MET amplification	Cancer Sci. 2018 May;109(5):1493-1502.
Nude mice	Non-small cell lung cancer patient-derived xenograft (PDX) models	Oral	15 mg/kg	5 days on, 2 days off for 4 cycles	To evaluate the efficacy of low-dose combination therapy in overcoming therapy resistance, results showed complete suppression of tumor growth in all PDX models	Commun Biol. 2022 Jan 17;5(1):59
CB17/lcr-PrkdcSCID/Crl mice	HCC1806 xenograft model	Oral gavage	10 mg/kg	5 days on, 2 days off, for 21-23 days	To evaluate the antitumor efficacy of afatinib combined with dasatinib in the HCC1806 xenograft model, the combination treatment significantly delayed tumor growth.	Ther Adv Med Oncol. 2020 Jan 28;12:1758835919897546.
NSG mice	SUIT2 orthotopic model	Intraperitoneal	5 mg/kg	Once daily for 10 days	Evaluate the antitumor efficacy of afatinib combined with MRTX1133, showing significant reduction in tumor volume	Cancer Res. 2023 Sep 15;83(18):3001-3012.

Afatinib dimaleate/双马来酸盐阿法替尼动物研究

Dose

Rat: 4 mg/kg^[3] (i.v.); 8 mg/kg^[3] (p.o.)

Administration

i.v., p.o.

Pharmacokinetics

Animal	Rats^[3]
Dose	4 mg/kg (i.v.) 8 mg/kg (p.o.)
Administration	i.v. p.o.
MRT	4.95 h (i.v.) 6.65 h (p.o.)
AUC_0→24h	2500 nmol·h/l (i.v.) 2540 nmol·h/l (p.o.)
T_1/2	5.22 h (i.v.) 4.54 h (p.o.)
T_max	4 h (p.o.)
V_z/F	25.0 L/kg (i.v.) 42.8 L/kg (p.o.)
C_max	1620 nmol/l (i.v.) 397 nmol/l (p.o.)
AUC_0→∞	2920 nmol·h/l (i.v.) 2600 nmol·h/l (p.o.)
V_ss/F	16.2 L/kg (i.v.) 43.6 L/kg (p.o.)
CL/F	55.3 ml/min·kg (i.v.) 108 ml/min·kg (p.o.)

Afatinib dimaleate/双马来酸盐阿法替尼参考文献

[1]Wang XK, He JH, et al. Afatinib enhances the efficacy of conventional chemotherapeutic agents by eradicating cancer stem-like cells. Cancer Res. 2014 Aug 15;74(16):4431-45.

[2]Li D, Ambrogio L, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11.

[3]Afatinib Dimaleate

Afatinib dimaleate/双马来酸盐阿法替尼实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.39mL

0.28mL

0.14mL

6.96mL

1.39mL

0.70mL

13.93mL

2.79mL

1.39mL

Afatinib dimaleate/双马来酸盐阿法替尼技术信息

CAS号	850140-73-7
分子式	C₃₂H₃₃ClFN₅O₁₁
分子量	718.08
SMILES Code	O=C(NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1O[C@@H]4COCC4)/C=C/CN(C)C.O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O
MDL No.	MFCD25974239

别名	马来酸阿法替尼 ;BIBW 2992MA2; Afatinib (maleate); BIBW 2992; BIBW2992 Dimaleate
运输	蓝冰

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: 35 mg/mL(48.74 mM)，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

H₂O: 50 mg/mL(69.63 mM)，配合低频超声助溶

动物实验：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

Afatinib dimaleate/双马来酸盐阿法替尼 {[allProObj[0].p_purity_real_show]}

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Afatinib dimaleate/双马来酸盐阿法替尼生物活性

Afatinib dimaleate/双马来酸盐阿法替尼细胞实验

Afatinib dimaleate/双马来酸盐阿法替尼动物实验

Afatinib dimaleate/双马来酸盐阿法替尼动物研究

Afatinib dimaleate/双马来酸盐阿法替尼参考文献

Afatinib dimaleate/双马来酸盐阿法替尼实验方案

Afatinib dimaleate/双马来酸盐阿法替尼技术信息

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EGFR/ErbB1	EGFR (wt), IC50:0.5 nM EGFR (L858R/T790M), IC50:0.4 nM
HER2/ErbB2	HER2, IC50:14 nM
HER2	HER2, IC50:14 nM

Afatinib dimaleate/双马来酸盐阿法替尼 {[allProObj[0].p_purity_real_show]}

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Afatinib dimaleate/双马来酸盐阿法替尼 质控信息

Afatinib dimaleate/双马来酸盐阿法替尼 生物活性

Afatinib dimaleate/双马来酸盐阿法替尼 细胞实验

Afatinib dimaleate/双马来酸盐阿法替尼 动物实验

Afatinib dimaleate/双马来酸盐阿法替尼 动物研究

Afatinib dimaleate/双马来酸盐阿法替尼 参考文献

Afatinib dimaleate/双马来酸盐阿法替尼 实验方案

Afatinib dimaleate/双马来酸盐阿法替尼 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Afatinib dimaleate/双马来酸盐阿法替尼纯度/质量文件产品仅供科研

Afatinib dimaleate/双马来酸盐阿法替尼质控信息

Afatinib dimaleate/双马来酸盐阿法替尼生物活性

Afatinib dimaleate/双马来酸盐阿法替尼细胞实验

Afatinib dimaleate/双马来酸盐阿法替尼动物实验

Afatinib dimaleate/双马来酸盐阿法替尼动物研究

Afatinib dimaleate/双马来酸盐阿法替尼参考文献

Afatinib dimaleate/双马来酸盐阿法替尼实验方案

Afatinib dimaleate/双马来酸盐阿法替尼技术信息