An inhibitor of VEGFRs (IC50s = 0.38

NVP-ACC789 – 1 mg

Brand:
Cayman
CAS:
300842-64-2
Storage:
-20
UN-No:
Non-Hazardous - /

NVP-ACC789 is an inhibitor of VEGF receptor tyrosine kinases (VEGFRs; IC50s = 0.38, 0.02, 0.18, and 0.23 μM for human VEGFR1, 2, 3, and mouse Vegfr2, respectively).{37221} It is selective for VEGFRs over FGFRs and PDGFRα (IC50s = >10 μM) but has activity at PDGFRβ (IC50 = 1.4 μM) in an enzyme assay. NVP-ACC789 inhibits VEGF-induced VEGFR2 autophosphorylation (IC50 = 11.5 nM in CHO cells transfected with the human receptor). It also inhibits VEGF- and bFGF-induced angiogenesis and cell migration of BAE and BME cells. In vivo, NVP-ACC789 blocks bFGF- and VEGF-induced angiogenesis (ED50s = 9 and 26 mg/kg, respectively) in a mouse model of growth factor-induced angiogenesis.  

 

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Description

An inhibitor of VEGFRs (IC50s = 0.38, 0.02, 0.18, and 0.23 μM for human VEGFR1, 2, 3, and mouse Vegfr2, respectively); selective for VEGFRs over FGFRs and PDGFRα (IC50s = >10 μM), but has activity at PDGFRβ (IC50 = 1.4 μM) in an enzyme assay; inhibits VEGF-induced VEGFR2 autophosphorylation (IC50 = 11.5 nM in CHO cells transfected with the human receptor); blocks bFGF- and VEGF-induced angiogenesis (ED50s = 9 and 26 mg/kg, respectively) in a mouse model of growth factor-induced angiogenesis

Formal name: N-(3-bromo-4-methylphenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine

Synonyms: 

Molecular weight: 405.3

CAS: 300842-64-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cell Biology|Cell Signaling|Growth Factor Receptors

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