1. Protein Tyrosine Kinase/RTK Apoptosis
  2. VEGFR Apoptosis
  3. 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.

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VEGFR-2-IN-73

VEGFR-2-IN-73 Chemical Structure

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Description

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[1].

IC50 & Target[1]

VEGFR-2

0.0787 μM (IC50)

In Vitro

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.

Cell Cycle Analysis[1]

Cell Line: HCT-116, HepG-2, and MCF-7 Cells
Concentration: 3.66, 3.31, and 4.29 μM for HCT-116, HepG-2, and MCF-7 Cells, respectively
Incubation Time: 72 h
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.

Apoptosis Analysis[1]

Cell Line: HCT-116, HepG-2, and MCF-7 Cells
Concentration: 3.66, 3.31, and 4.29 μM for HCT-116, HepG-2, and MCF-7 Cells, respectively
Incubation Time: 72 h
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.
Molecular Weight

559.70

Formula

C29H29N5O3S2

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

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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  • 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.

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Product Name:
VEGFR-2-IN-73
Cat. No.:
HY-178004
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