产品说明
生化/生理作用
Afatinib (BIBW2992) is an orally active, irreversible, potent and selective EGFR/HER2 (ErbB2) dual inhibitor (EGFR IC50 = 0.5 nM (Wt), 0.4 nM (L858R), 10 nM (L858R/T790M); HER2 IC50 = 14 nM) that covalently targets EGFR Cys773 and HER2 Cys805 residues. BIBW2992 suppresses 100 ng/mL EGF-induced EGFR/HER2 tyrosin phosphorylation (IC50 = 13-71 nM; A431, NIH-3T3-HER2, BT-474, NCI-N87), inhibits cancer cells survival in cultures and induces tumor regression in xenograft and transgenic lung cancer models in vivo (20 mg/kg/day p.o.).
基本信息
经验(实验)分子式 | C32H33ClFN5O11 |
分子量 | 718.08 |
MDL编号 | MFCD25974239 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
颜色 | white to beige |
溶解性 | H2O: 2 mg/mL, clear |
储存温度 | 2-8℃ |
SMILES string | OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O.CN(C)C/C=C/C(NC1=CC(C(NC2=CC=C(F)C(Cl)=C2)=NC=N3)=C3C=C1O[C@H]4CCOC4)=O |
安全信息
象形图 | |
警示用语: | Warning |
危险声明 | H302 - H319 - H373 |
预防措施声明 | P260 - P264 - P270 - P301 + P312 - P305 + P351 + P338 - P314 |
危险分类 | Acute Tox. 4 Oral - Eye Irrit. 2 - STOT RE 2 |
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich