VEGFR-2-IN-88
VEGFR-2-IN-88 is a VEGFR-2 inhibitor with an IC50 of 0.202 μM. VEGFR-2-IN-88 potently inhibits EGFR (IC50 = 0.139 μM), and moderately inhibits PDGFR-β (IC50 of 0.236 μM) and c-Met (IC50 of 0.281 μM). VEGFR-2-IN-88 acts as a cell cycle inhibitor that arrests cells at the G0/G1 phase. VEGFR-2-IN-88 induces Apoptosis. VEGFR-2-IN-88 downregulates serum AST and ALT levels. VEGFR-2-IN-88 exerts selective anticancer effects. VEGFR-2-IN-88 reduces liver weight in in vivo models. VEGFR-2-IN-88 can be used in research related to hepatocellular carcinoma.
For research use only. We do not sell to patients.
- Formula: C22H17N5O2
- Molecular Weight:383.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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VEGFR2 0.202 μM (IC50) |
EGFR 0.139 μM (IC50) |
PDGFR-β 0.236 μM (IC50) |
c-Met 0.281 μM (IC50) |
VEGFR-2-IN-88 (Compound 6a) potently inhibits the proliferation of HepG-2, Hep-2, PC-3, HeLa, HCT-116 and MCF-7 cells, with the strongest activity against HepG-2 cells (IC50 = 3.56 μM)[1].
VEGFR-2-IN-88 inhibits the tyrosine kinase activity of VEGFR-2, with an IC50 of 0.202 μM[1].
VEGFR-2-IN-88 is a multi-kinase inhibitor that potently inhibits EGFR (IC50 = 0.139 μM) and moderately inhibits PDGFR-β and c-Met[1].
VEGFR-2-IN-88 exhibits low cytotoxicity against normal cells WI-38 and L02, and shows high selectivity toward HepG-2 cancer cells (with SI values of 9.58 and 9.66, respectively)[1].
VEGFR-2-IN-88 (24 h) arrests hepatocellular carcinoma cells HepG-2 at the G0/G1 phase of the cell cycle[1].
VEGFR-2-IN-88 (24 h) induces apoptosis in hepatocellular carcinoma HepG-2 cells, with a total apoptosis rate of 29.31%[1].
VEGFR-2-IN-88 regulates the expression of apoptosis-related proteins in hepatocellular carcinoma HepG-2 cells, upregulating the levels of caspase-3 and Bax while downregulating the level of Bcl-2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG-2
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Concentration:IC50 concentration
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Incubation Time:24 h
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Result:Increased the proportion of HepG-2 cells in G0/G1 phase from 52.61% (control) to 77.26%.
Decreased the proportion of HepG-2 cells in S phase from 36.04% to 19.28%.
Decreased the proportion of HepG-2 cells in G2/M phase from 11.35% to 3.46%.
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Cell Line:HepG-2
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Concentration:IC50 concentration
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Incubation Time:24 h
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Result:Increased total apoptosis (early + late) of HepG-2 cells to 29.31% compared to 0.93% in untreated control cells.
Resulted in a necrotic cell proportion of only 5.41%, indicating cell death is primarily mediated by apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 383.40
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Formula C22H17N5O2
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SMILES
O=C(N/N=C/C1=CC=CC=C1)C2=CC=C(N/N=C3C(NC4=C\3C=CC=C4)=O)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VEGFR-2-IN-88 Related Classifications
HY-184719 Related Classifications
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