2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. 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.

VEGFR-2-IN-80

VEGFR-2-IN-80 Chemical Structure

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VEGFR-2-IN-80 Related Antibodies

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Description

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[1].

IC50 & Target

VEGFR2

2.206 μM (IC50)

In Vitro

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.

VEGFR-2-IN-80 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: SKOV3, HT29, HCT116, DU145, 22Rv1, A549, MCF7, Mel P, SK-MEL28, SW620, HEK293
Concentration: 6.25-200 μM
Incubation Time: 72 h
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.
In Vivo

VEGFR-2-IN-80 (SA7) (25-50 mg/kg; p.o.; daily; 21 days) exhibits dose-dependent antitumor efficacy in HCT116 xenograft mice, with 50 mg/kg achieving 65.5% tumor growth inhibition[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (male, 6-8 weeks old, 22 ± 2 g, HCT116 xenograft model)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: p.o.; daily; 21 days
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.
Molecular Weight

534.51

Formula

C27H17F3N4O3S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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VEGFR-2-IN-80 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VEGFR-2-IN-80VEGFRVascular endothelial growth factor receptorcolorectal cancerHEK293 cellsHUVEC cellsHT29ATP-binding residueskinase activitySKOV3VEGFR-2HCT116 xenograftshuman cancer cellsInhibitorinhibitorinhibit

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