A potent inhibitor of VEGFR2 and bFGF (IC50s = 11 and 9 nM

CP 547,632 – 5 mg

Brand:
Cayman
CAS:
252003-65-9
Storage:
4
UN-No:
Non-Hazardous - /

CP 547,632 is an orally bioavailable and potent inhibitor of the receptor tyrosine kinases VEGF receptor 2 (VEGFR2) and basic fibroblast growth factor (bFGF) with IC50 values of 11 and 9 nM, respectively, in an enzyme assay.{38241} It is selective for VEGFR2 and bFGF over EGFR, PDGF receptor β (PDGFRβ), and related tyrosine kinases. CP 547,632 inhibits VEGFR2 autophosphorylation induced by VEGF in porcine aortic endothelial cells transfected with VEGFR2 (IC50 = 6 nM) and in a xenograft mouse model using NIH3T3/H-Ras cells (EC50 = 590 nM). It decreases angiogenesis induced by VEGF or bFGF and suppresses tumor growth in athymic mice.  

 

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Description

A potent inhibitor of VEGFR2 and bFGF (IC50s = 11 and 9 nM, respectively); selective over EGFR, PDGRβ, and related tyrosine kinases; inhibits VEGFR2 autophosphorylation induced by VEGF in vitro (IC50 = 6 nM) and in a xenograft mouse model (EC50 = 590 nM); decreases angiogenesis induced by VEGF or bFGF; suppresses tumor growth in athymic mice ,

Formal name: 3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-[[[[4-(1-pyrrolidinyl)butyl]amino]carbonyl]amino]-4-isothiazolecarboxamide

Synonyms: 

Molecular weight: 532.4

CAS: 252003-65-9

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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