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448104 c-Met/RON Dual Kinase Inhibitor - CAS 913376-84-8 - Calbiochem

448104
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Panoramica

Replacement Information

Tabella delle specifiche principali

Empirical FormulaCAS #
C₃₁H₂₉FN₄O₅ 913376-84-8

Products

Numero di catalogoConfezionamento Qtà/conf
448104-5MG Fiala di plastica 5 mg
Description
OverviewA 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.
Catalogue Number448104
Brand Family Calbiochem®
SynonymsN-(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, Met Kinase Inhbitor IV, Ron Inhibitor I
References
ReferencesZhang, Y., et al. 2008. Cancer Res. 68, 6680.
Product Information
CAS number913376-84-8
FormLight tan solid
Hill FormulaC₃₁H₂₉FN₄O₅
Chemical formulaC₃₁H₂₉FN₄O₅
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

c-Met/RON Dual Kinase Inhibitor - CAS 913376-84-8 - Calbiochem MSDS

Titolo

Scheda di sicurezza (MSDS) 

c-Met/RON Dual Kinase Inhibitor - CAS 913376-84-8 - Calbiochem Certificati d'Analisi

TitoloNumero di lotto
448104

Riferimenti bibliografici

Panoramica delle referenze
Zhang, Y., et al. 2008. Cancer Res. 68, 6680.
Scheda tecnica

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision13-April-2011 RFH
SynonymsN-(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, Met Kinase Inhbitor IV, Ron Inhibitor I
DescriptionA 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.
FormLight tan solid
Intert gas (Yes/No) Packaged under inert gas
CAS number913376-84-8
Chemical formulaC₃₁H₂₉FN₄O₅
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (40 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesZhang, Y., et al. 2008. Cancer Res. 68, 6680.