The Met/Flt-3/VEGFR2 Tyrosine Kinase Inhibitor controls the biological activity of Met/Flt-3/VEGFR2 Tyrosine Kinase. Primarily used for Phosphorylation & Dephosphorylation applications.
A cell-permeable pyrrolopyridine-pyridone compound that acts as a potent ATP-competitive inhibitor of Met, Flt-3 and VEGFR2 (IC50 = 1.9, 4.0 and 27 nM, respectively), while exhibiting much reduced potency against Lck and c-Kit (IC50 = 290 and 610 nM, respectively) and little or no activity agaisnt Cdk2/CycE, IGF-1R, InsR, MK-2, PKA, and PKCα (IC50 >1 µM). Shown to selectively inhibit the Met-dependent, but not Met-independent, proliferation of gastric carcinoma cultures (IC50 = 60 nM vs. >5 µM against GTL-6 and N87 cells, respectively) in vitro and effectively abolish GTL-6-derived tumor growth (110% reduction of control tumor mass 39 days after tumor implant) by daily oral dosing (50 mg/kg) in mice in vivo.
包裝
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重構
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他說明
Kim, K.S., et al. 2008. J. Med. Chem.51, 5330.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany