448103
Met/Flt-3/VEGFR2 Tyrosine Kinase Inhibitor
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.
别名:
Met/Flt-3/VEGFR2 Tyrosine Kinase Inhibitor, N-(4-(1H-Pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorophenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide, Flt-3 Inhibitor VI, VEGFR Tyrosine Kinase Inhibitor XXVI, VEGFR2 Kinase Inhibitor XXIV
InChI
1S/C25H16F2N4O3/c26-15-3-6-17(7-4-15)31-13-1-2-19(25(31)33)24(32)30-16-5-8-22(20(27)14-16)34-21-10-12-29-23-18(21)9-11-28-23/h1-14H,(H,28,29)(H,30,32)
InChI key
OBSFXHDOLBYWRJ-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white to beige, white
solubility
ethanol: 1 mg/mL, DMSO: 10 mg/mL
shipped in
ambient
Quality Level
General description
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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Kim, K.S., et al. 2008. J. Med. Chem.51, 5330.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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