877399-52-5

PF-2341066(Crizotinib)

877399-52-5

Cat.No.ABP000131 Chemical NamePF-2341066(Crizotinib) MDL: MFCD00043011 MolFormulaC21H22Cl2FN5O MolWeight450.337 Purity >99%

Chemical Name : PF-2341066(Crizotinib)

CAS : 877399-52-5

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

Solubility:Soluble in DMSO and in water

Storage:Storage at -20C 2 years

Biologieal

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).

Reference

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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