Crizotinib, Free Base **

产品名称：Crizotinib, Free Base
产品货号：LC  C-7900
产品规格：10 MG
Crizotinib, also known as PF-02341066, is a potent ATP-competitive, recombinant human c-Met kinase inhibitor (Ki = 4 nM).  In cell-based assays, it inhibited hepatocyte growth factor (HGF)-stimulated or constitutive total tyrosine phosphorylation of wild-type c-Met in a panel of human tumor and endothelial cell lines.  It showed activity against c-Met phosphorylation in mIMCD3 mouse (IC50 = 5 nM) or MDCK canine (IC50 = 20 nM) epithelial cells.  Crizotinib inhibited human GTL-16 gastric carcinoma cell growth (IC50 = 9.7 nM), induced apoptosis in GTL-16 cells (IC50 = 8.4 nM), inhibited HGF-stimulated human NCI-H441 lung carcinoma cell migration and invasion (IC50s of 11 and 6.1 nM, respectively), and inhibited MDCK cell scattering (IC50 = 16 nM).  Crizotinib also inhibited HGF-stimulated c-Met phosphorylation (IC50 = 11 nM), cell survival (IC50 = 14 nM), and Matrigel invasion (IC50 = 35 nM) in human umbilical vascular endothelial cells.  In addition, it inhibited serum-stimulated human dermal microvascular endothelial cell branching tubulogenesis (formation of vascular tubes) in fibrin gels.  Crizotinib showed antitumor effects in vivo in c-Met-dependent human xenograft models including GTL-16 human gastric carcinoma, U87MG human glioblastoma, NCI-H441 NSCLC, Caki-1 RCC, and PC-3 prostate carcinoma.  Zou, H.Y., et al.  "An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms."  Cancer Res. 67:  4408-4417 (2007).
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 25 mg/mL with warming; soluble in ethanol at 25 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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