BIBW2992 (Afatinib)

Catalog No. A10141

BIBW2992 (Afatinib)是酪氨酸激酶抑制剂（TKI），它不可逆地抑制人表皮生长因子受体2（Her2）和表皮生长因子受体（EGFR）激酶。

Product Citations

Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
Van Sebille YZ, .et al. Use of zebrafish to model chemotherapy and targeted therapy gastrointestinal toxicity, Exp Biol Med (Maywood), 2019, Jun 11:1535370219855334 PMID: 31184924
Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358

Technical details

Catalog Num	A10141
M. Wt	485.9
Formula	C24H25ClFN5O3
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	439081-18-2
Synonyms	Tomtovok,Afatinib
SMILES	CN(C)C/C=C/C(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)O[C@H]4CCOC4

Biological Activity

BIBW2992 (Afatinib)是酪氨酸激酶抑制剂（TKI），它不可逆地抑制人表皮生长因子受体2（Her2）和表皮生长因子受体（EGFR）激酶。

Targets

EGFR (L858R) (Cell-free assay)	EGFR (wt) (Cell-free assay)	EGFR (L858R/T790M) (Cell-free assay)	HER2 (Cell-free assay)
0.4 nM	0.5 nM	10 nM	14 nM

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	20.58 mL	102.9 mL	205.8 mL
0.5 mM	4.12 mL	20.58 mL	41.16 mL
1 mM	2.06 mL	10.29 mL	20.58 mL
5 mM	0.41 mL	2.06 mL	4.12 mL

*The above data is based on the productmolecular weight 485.9. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.