AZD9291

英文名		AZD-9291 mesylate
别名		N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide methanesulfonate (1:1)
产品名称		AZD-9291 甲磺酸盐
分子结构
分子式		C28H33N7O2.CH4O3S
分子量		595.71
CAS 登录号		1421373-66-1

AZD-9291 mesylate的生物活性

AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).
IC50 value: 12.92 nM(Exon 19 deletion EGFR); 11.44 nM(L858R/T790M EGFR) [1]
Target: L858R/T790M EGFR; Exon 19 deletion EGFR
AZD-9291 is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. AZD9291 is highly active in preclinical models and is well tolerated in animal models. It inhibits both activating and resistant EGFR mutations while sparing the normal form of EGFR that is present in normal skin and gut cells, thereby reducing the side effects encountered with currently available medicines.
Patent: WO 2013014448