Ki8751 – 50 mg

Brand:
Cayman
CAS:
228559-41-9
Storage:
-20
UN-No:
Non-Hazardous - /

Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. Ki8751 is a potent, orally available inhibitor of the kinase activity of VEGFR2 (IC50 = 0.9 nM).{31021} It less potently inhibits c-Kit, PDGRFα, and FGFR2 (IC50s = 40-170 nM) and has no significant effect against several other receptor tyrosine kinases. Ki8751 suppresses the growth of VEGF-stimulated human umbilical vein endothelial cells at nanomolar concentrations.{31021} It shows significant anti-tumor activity against assorted human tumor xenografts in nude mice.{31021} Ki8751 also induces cellular senescence in colorectal cancer cells.{31020}  

 

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Description

A potent, orally available inhibitor of the kinase activity of VEGFR2 (IC50 = 0.9 nM); suppresses the growth of VEGF-stimulated HUVECs at nanomolar concentrations; shows significant anti-tumor activity against assorted human tumor xenografts in nude mice


Formal name: N-(2,4-difluorophenyl)-N’-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]-urea

Synonyms: 

Molecular weight: 469.4

CAS: 228559-41-9

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cell Biology|Cell Signaling|Growth Factor Receptors