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

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双马来酸盐阿法替尼 /Afatinib dimaleate 98%

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 化学结构
CAS号：850140-73-7

Afatinib dimaleate 3D分子结构
CAS号：850140-73-7

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Afatinib dimaleate 纯度/质量文件产品仅供科研

货号：A170920 标准纯度： 98% 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: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 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					PKA,PKC	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		96%
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					VEGFR,Src	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						98%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		98%
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	✔						98%
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	++ L858R/T790M EGFR, IC50: 11.44 nM WT EGFR, IC50: 12.92 nM						99%
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						98+%
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						98%
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		98+%
Lazertinib	++++ L858R/T790M EGFR, IC50: 2 nM WT EGFR, IC50: 76 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	97%
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	✔						99%
(S)-Sunvozertinib	✔						98%
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				✔			98%
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			98+%
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	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^T790M, IC50: 0.79 nM EGFR^L858R/T790M, IC50: 0.51 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			99+%
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		Raf,Src	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 dihydrochloride	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			98%
Allitinib tosylate	++++ EGFR, IC50: 0.5 nM EGFR (T790M/L858R), IC50: 12 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			98%
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			98%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			98%
ALK-IN-1					++ EGFR(C797S/del19), IC50: 138.6 nM EGFR(del19), IC50: 36.8 nM	ALK	98+%
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					✔		98%
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		98%
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	✔		98%
Canertinib	+++ ErbB2, IC50: 9.0 nM	EGFR	99%+
(E/Z)-CP-724714	++ HER2/ErbB2, IC50: 10 nM		98+%
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		99+%
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	✔		95%
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 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 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 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 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 技术信息

CAS号	850140-73-7
分子式	C₃₂H₃₃ClFN₅O₁₁
分子量	718.083

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

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

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

动物实验配方

5% DMSO+30% PEG 300+water 28 mg/mL suspension

双马来酸盐阿法替尼 /Afatinib dimaleate 98%

Afatinib dimaleate 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Afatinib dimaleate 质控信息

Afatinib dimaleate 生物活性

Afatinib dimaleate 动物研究

Afatinib dimaleate 参考文献

Afatinib dimaleate 实验方案

Afatinib dimaleate 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

双马来酸盐阿法替尼 /Afatinib dimaleate 98%

Afatinib dimaleate 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Afatinib dimaleate 质控信息

Afatinib dimaleate 生物活性

Afatinib dimaleate 动物研究

Afatinib dimaleate 参考文献

Afatinib dimaleate 实验方案

Afatinib dimaleate 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 纯度/质量文件产品仅供科研