VEGFR-2-IN-71
VEGFR-2-IN-71 is a dual VEGFR2/tubulin inhibitor. VEGFR-2-IN-71 inhibits tumor cell proliferation and induces apoptosis and cell cycle arrest. VEGFR-2-IN-71 inhibits angiogenesis in the chick chorioallantoic membrane (CAM) model. VEGFR-2-IN-71 inhibits tumor growth in the HGC-27 xenograft model by inhibiting VEGFR2 and tubulin. VEGFR-2-IN-71 has low oral bioavailability in rats. VEGFR-2-IN-71 can be used in cancer research.
For research use only. We do not sell to patients.
- Formula: C26H20F4N2O6
- Molecular Weight:532.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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Biological Activity
VEGFR-2-IN-71 (Compound 6r) (1-128 μM, 48 hours) exhibits antitumor activity and cytotoxicity against HepG-2, HCT-116, HGC-27, MDA-MB-231, MCF-7, HA-VSMC, and GES-1 cells with IC50 values of 13.3 μM, 18.8 μM, 11.4 μM, 21.8 μM, 17.4 μM, 17.1 μM, and 16.73 μM, respectively[1].
VEGFR-2-IN-71 (0-2 μM, 24-72 hours) exhibits antiproliferative effects against HGC-27 and HepG-2 cells, achieving complete inhibition at 1.0 μM[1].
VEGFR-2-IN-71 (0-1 μM, 10 days) inhibits colony formation of HGC-27 and HepG-2 cells[1].
VEGFR-2-IN-71 (0-1 μM) inhibits VEGFR2 activity and exerts anti-tumor effects in HGC-27 cells by downregulating VEGF expression and regulating glycolysis-related enzymes HK2, PFKM, and PKM2[1].
VEGFR-2-IN-71 (0-1 μM) inhibits tubulin polymerization and disrupts microtubule dynamics in HGC-27 and HepG-2 cells[1].
VEGFR-2-IN-71 (0-1 μM) induces cell cycle arrest and apoptosis in HGC-27 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HGC-27 cells
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Concentration:0 μM, 0.25 μM, 0.5 μM , 1 μM
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Incubation Time:/
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Result:Reduced VEGF protein expression.
Inhibited hexokinase 2 (HK2), phosphofructokinase muscle (PFKM) and pyruvate kinase M2 (PKM2) protein expression.
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Cell Line:HGC-27 cells
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Concentration:0 μM, 0.25 μM, 0.5 μM , 1 μM
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Incubation Time:/
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Result:Induced cell cycle arrest at the G2/M phase and apoptosis, with the percentages of apoptotic cells at 0.25, 0.5, and 1 μM were 10.01%, 13.45%, and 16.54%, respectively.
VEGFR-2-IN-71 (15-30 mg/kg, intraperitoneal injection, once every other day, for 16 days) exerts antitumor activity and angiogenesis inhibition in BALB/c nude mice bearing HGC-27 xenograft tumors[1].
VEGFR-2-IN-71 (20-100 mg/kg, intraperitoneal injection, once a day, for 12 days) does not damage the heart, liver, spleen, lung or kidney, and does not cause death, showing a good safety profile[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (15-18 g, 5 weeks old) bearing HGC-27 xenografts model (4 × 106 cells subcutaneously implanted in the left armpit) [1]
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Dosage:15 mg/kg, 30 mg/kg
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Administration:i.p., every other day, 16 days
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Result:Inhibited tumor growth at 15 mg/kg, reduced the growth rates and final weights of tumors, showing an inhibitory effect on tumor growth, with the rates reaching 68.35% at 30 mg/kg.
Reduced the expression of Ki67 and MVD and inhibited angiogenesis within tumors.
Reduced the levels of VEGFA, a marker of angiogenesis, and VEGFR-2, an early marker of endothelial progenitor cells, in tumors.
Chemical Information
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Molecular Weight 532.44
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Formula C26H20F4N2O6
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SMILES
COC1=C(OC)C(OC)=C(C(C=C(C2=CC=C(NC(NC3=CC=C(F)C(C(F)(F)F)=C3)=O)C=C2)O4)=O)C4=C1
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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-71 Related Classifications
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