877399-52-5

PF-2341066(Crizotinib)

877399-52-5

编号ABP000131 化学名称PF-2341066(Crizotinib) 英文名称 PF-2341066(Crizotinib) MDL: MFCD00043011 分子式C21H22Cl2FN5O 分子量450.337 纯度 >99%

化学名称 : PF-2341066(Crizotinib)

CAS : 877399-52-5

英文名称: PF-2341066(Crizotinib)

英文同义词: (R)-3-(1-(2,6-Dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine

溶解度:Soluble in DMSO and in water

储存条件:Storage at -20C 2 years

生物活性

PF-2341066(Crizotinib) was shown to be a potent ATP-competitive inhibitor of c-Met kinase with a Ki=4 nmol/L and IC50 value of 11 nmol/L across a panel of human tumor and endothelial cell lines. PF-2341066(Crizotinib) showed similar potency against c-Met phosphorylation in mIMCD3 mouse (IC50, 5 nmol/L) or MDCK canine (IC50, 20 nmol/L) epithelial cells. PF-2341066(Crizotinib) exhibited improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I (IC50, 19 nmol/L) or H1094R (IC50, 2 nmol/L) or the P-loop mutant M1250T (IC50, 15 nmol/L) compared with NIH3T3 cells expressing wild-type receptor (IC50, 13 nmol/L).

参考文献

Intermediates of Crizotinib(Indication:Advancedormetastaticnon-smallcelllungcancer) 4-(4-Bromopyrazol-1-yl)piperidine-1-carboxylic acid tert-butyl ester 877399-50-3 and (R)-5-bromo-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine cas 877399-00-3
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