c-Met/RON Dual Kinase Inhibitor

货号： 448104-5MG      产品名称： c-Met/RON Dual Kinase Inhibitor   品牌： Merck 规格： *** 3周到货 生化实验

c-Met/RON Dual Kinase Inhibitor
N-(3-Fluoro-4-(7-methoxy-4-quinolinyl)phenyl)-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-phenyl-2,3-dihydro-1H-pyrazole carboxamide, Compound I, Met Kinase Inhbitor IV, Ron Inhibitor I
A cell-permeable quinoline compound that acts as a potent inhibitor against the kinase activities of HGF (Cat. No. 375228) receptor c-Met and MSP (Macrophage Stimulating Protein) receptor RON (IC50 = 4 and 9 nM, respectively), while exhibiting much weaker potency toward Lck, Tie2, Src, BTK, IGFR, or VEGFR2 (IC50 = 160, 400, 410, 710, 1000, and 1900 nM, respectively), and little or no activity against B-Raf and more than 20 other kinases IC50 >1 µM). Shown to effectively supress (IC50 <100 nM) the ligand-induced autophosphorylations of wild-type c-Met (in HT-29 and BxPC3 cultures) and RON (in NIH3T3 RON and BxPC3 cultures) as well as the ligand-independent autophosphorylations of the constitutively active mutants TPR-Met and RONΔ160 (in NIH3T3 TRP-Met and HT-29 cultures, respectively). Reported to inhibit NIH3T3 TRP-Met and U-87 tumor growth in mice in vivo in a dose-dependent manner (complete inhibition via daily p.o. dose of 100 mg/kg), but is less efficacious against HT-29, whose in vivo tumor growth is also dependent on V600E B-raf.
产品信息
Form  Light tan solid
Molar mass  556.6
Protect from Light  是的
Packaged under inert gas  是的
Purity  ≥95% by HPLC
Solubility  DMSO
Chemical formula  C31H29FN4O5
CAS number  913376-84-8
商店和运输信息
Storage  +2°C to +8°C
Ship  Ambient Temperature Only
Standard Handling

2°C – 8°C