448103

Sigma-Aldrich

Met/Flt-3/VEGFR2 Tyrosine Kinase Inhibitor - CAS 888719-03-7 - Calbiochem

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.

Synonym(s):
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, Met/Flt-3/VEGFR2 Tyrosine Kinase Inhibitor - CAS 888719-03-7 - Calbiochem
Empirical Formula (Hill Notation):
C25H16F2N4O3
CAS Number:
Molecular Weight:
458.42
Pricing and availability is not currently available.

storage conditions

+2C to +8C

Quality Level

assay

≥95% (HPLC)

form

solid

mfr. no.

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

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

5 mg in Plastic ampoule
Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

WGK Germany

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis
Certificate of Origin

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