VEGFR-2-IN-80
VEGFR-2-IN-80 is a VEGFR-2 inhibitor with an IC50 of 2.206 μM. VEGFR-2-IN-80 interacts with ATP-binding residues of VEGFR-2 to inhibit its kinase activity. VEGFR-2-IN-80 suppresses formation of capillary-like networks, exerts cytotoxic effects against various human cancer cells, and suppresses growth of HCT116 xenografts. VEGFR-2-IN-80 can be used for the research of colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C27H17F3N4O3S
- Molecular Weight:534.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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VEGFR2 2.206 μM (IC50) |
VEGFR-2-IN-80 (SA7) (2 μM; 30 min) inhibits VEGFR-2 in HUVEC cells with an IC50 of 2.206 μM[1].
VEGFR-2-IN-80 (6.25-200 μM; 72 h) shows broad-spectrum cytotoxicity against human cancer cell lines (SKOV3, HT29, HCT116, etc.) with low-micromolar IC50 values and reduced activity in non-cancerous HEK293 cells[1].
VEGFR-2-IN-80 (Non-cytotoxic concentrations; 30 min pre-incubation, 16 h Matrigel incubation) inhibits capillary-like network formation in HUVEC cells with 44.89% inhibition at non-cytotoxic concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKOV3, HT29, HCT116, DU145, 22Rv1, A549, MCF7, Mel P, SK-MEL28, SW620, HEK293
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Concentration:6.25-200 μM
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Incubation Time:72 h
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Result:Exhibited low-micromolar cytotoxicity across various cancer cell lines, with IC50 values of 5.6 μM (SKOV3), 9.3 μM (HT29), 11.3 μM (HCT116), 14.5 μM (DU145), 16.6 μM (22Rv1), 15.7 μM (A549), 15.4 μM (MCF7), 13.4 μM (Mel P), 11.4 μM (SK-MEL28), and 13.6 μM (SW620); showed reduced activity in HEK293 cells with an IC50 of 46.8 μM.
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 (male, 6-8 weeks old, 22 ± 2 g, HCT116 xenograft model)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:p.o.; daily; 21 days
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Result:Reduced average tumor volume to 1690 mm3 (TGI 47%) versus control at 25 mg/kg; reduced average tumor volume to 1094 mm3 (TGI 65.5%) versus control at 50 mg/kg.
Chemical Information
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Molecular Weight 534.51
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Formula C27H17F3N4O3S
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SMILES
FC1=CC(F)=CC2=C1N=C(S2)NC(COC3=CC(C=C4)=C(C=C3)C=C4/C=N/NC(C5=CC=C(F)C=C5)=O)=O
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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-80 Related Classifications
HY-181173 Related Classifications
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