| Identification | Back Directory | [Name]
VEGFR2 Kinase Inhibitor II | [CAS]
288144-20-7 | [Synonyms]
VEGFR2 Kinase Inhibitor II
VEGFR2 Kinase Inhibitor II,VEGFR-2 Kinase Inhibitor II
VEGFR2 Kinase Inhibitor II - CAS 288144-20-7 - Calbiochem
(3Z)-5-bromo-3-(4,5,6,7-tetrahydro-1H-indol-2-ylmethylidene)-1H-indol-2-one
2H-Indol-2-one, 5-bromo-1,3-dihydro-3-[(4,5,6,7-tetrahydro-1H-indol-2-yl)methylene]-, (3Z)- | [Molecular Formula]
C17H15BrN2O | [MDL Number]
MFCD03453583 | [MOL File]
288144-20-7.mol | [Molecular Weight]
343.22 |
| Hazard Information | Back Directory | [Uses]
VEGFR-2-IN-44 (compound 4b) is a selective VEGF-R2 (Flk-1) inhibitor with an IC50 value of 70 nM. VEGFR-2-IN-44 also inhibits PDGF-Rβ with an IC50 of 920 nM[1]. | [General Description]
A cell-permeable and reversible indolin-2-one class of receptor tyrosine kinase (RTK) inhibitor [IC50 = 70 nM for VEGF-R2 (KDR/Flk-1), 920 nM for PDGF-Rβ, 4.92 μM for p60c-src, and 13.3 μM for FGF-R1]. The inhibition is suggested to be competitive with respective to ATP. Also inhibits VEGF-induced (IC50 = 110 nM) and PDGF-induced (IC50 = 2.01 μM) cell proliferation in umbilical vein endothelial cells (HUVEC). Does not exhibit any inhibitory effect on EGF-R kinase activity (IC50 >100 μM). | [Biochem/physiol Actions]
Cell permeable: yes | [IC 50]
Flk-1: 70 nM (IC50); PDGFR-β: 920 nM (IC50) | [References]
[1] L Sun, et al. Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases. J Med Chem. 2000 Jul 13;43(14):2655-63. DOI:10.1021/jm9906116 |
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