VEGFR-2-IN-73
VEGFR-2-IN-73 is a potent and selective VEGFR-2 inhibitor, showing selectively inhibition of VEGFR-2 (IC50 = 0.0787 μM) over EGFR (IC50 = 1.31 μM). VEGFR-2-IN-73 demonstrates potent antiproliferative activity across multiple cancer cell lines. VEGFR-2-IN-73 induces G2/M and Pre-G1 phase arrest and significantly enhances apoptosis. VEGFR-2-IN-73 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer.
For research use only. We do not sell to patients.
- Formula: C29H29N5O3S2
- Molecular Weight:559.70
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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
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Biological Activity
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VEGFR-2 0.0787 μM (IC50) |
VEGFR-2-IN-73 (compound 15) (2 days) displays strong cytotoxicity against HCT-116, HepG-2, and MCF-7 Cell Lines (IC50 = 3.66, 3.31, and 4.29 μM, respectively), while showing minimal cytotoxicity against normal WI-38 cells (IC50 > 69 μM), demonstrating a favorable selectivity profile[1].
VEGFR-2-IN-73 (3.31-4.29 μM, 72 h) effectively induces cell cycle arrest at both the G2/M and Pre-G1 phases, and significantly triggers apoptosis in HCT-116, HepG-2, and MCF-7 Cells, with effects comparable to those of Doxorubicin (HY-15142A)[1].
VEGFR-2-IN-73 possesses a superior binding affinity for VEGFR-2 (predicted binding energy: -24.27 kcal/mol) compared to the reference inhibitor Sorafenib (HY-10201) (-20.88 kcal/mol)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116, HepG-2, and MCF-7 Cells
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Concentration:3.66, 3.31, and 4.29 μM for HCT-116, HepG-2, and MCF-7 Cells, respectively
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Incubation Time:72 h
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Result:Induced a significant increase in the Hep-G2 cell population in the G2/M (from 12.73% to 38.49%) and Pre-G1 (from 1.92% to 22.80%) phases.
Induced a significant increase in the HCT-116 cell population in the G2/M (from 5.45% to 22.72%) and Pre-G1 (from 1.91% to 16.05%) phases.
Significantly increased the population of MCF-7 Cells in the G2/M and Pre-G1 phases from 9.55% and 2.14% to 31.58% and 14.29%, respectively.
Reduced the proportion of cells in the G0-G1 and S phases compared to the control in Hep-G2, HCT-116, and MCF-7 cell lines.
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Cell Line:HCT-116, HepG-2, and MCF-7 Cells
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Concentration:3.66, 3.31, and 4.29 μM for HCT-116, HepG-2, and MCF-7 Cells, respectively
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Incubation Time:72 h
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Result:Induced a total apoptosis rate of 16.05% in HCT-116 cells (early: 5.64%; late: 8.72%).
Induced a total apoptosis rate of 22.8% in HepG-2 cells (early: 6.38%; late: 13.9%).
Induced a total apoptosis rate of 14.29% in MCF-7 cells (early: 5.86%; late: 6.77%).
Triggered apoptosis in HCT-116, HepG-2, and MCF-7 Cells, with an efficacy comparable to Doxorubicin.
Chemical Information
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Molecular Weight 559.70
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Formula C29H29N5O3S2
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SMILES
C/C(C1=CC=C(C=C1)S(=O)(N2CCC(CC2)C)=O)=N/N=C3SC(C(C4=CC=CC=C4)=O)=NN\3C5=CC=CC=C5
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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-73 Related Classifications
HY-178004 Related Classifications
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