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.

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₂₅H₁₆F₂N₄O₃
• CAS Number: 888719-03-7
• Molecular Weight: 458.42
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• 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
• storage temp.: 2-8°C
• 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

Description

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

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable