448104

c-Met/RON Dual Kinase Inhibitor

The c-Met/RON Dual Kinase Inhibitor, also referenced under CAS 913376-84-8, controls the biological activity of c-Met/RON.

• Synonyme(s) : c-Met/RON Dual Kinase Inhibitor, Met Kinase Inhbitor IV, Ron Inhibitor I, 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
• Formule empirique (notation de Hill): C₃₁H₂₉FN₄O₅
• Numéro CAS: 913376-84-8
• Poids moléculaire : 556.58
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Essai: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: light tan
• Solubilité: DMSO: 40 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C

Description

Description générale

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.

A cell-permeable quinoline compound that acts as a potent inhibitor against the kinase activities of HGF 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 M). 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.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Zhang, Y., et al. 2008. Cancer Res.68, 6680.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable