VEGFR2-IN-1 

VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC₅₀=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition^[1].

VEGFR2-IN-1 (compound 17; 0.1, 1, 10, 100 μM; 48 hours) shows an effective and selective agent against MCF-7 (IC₅₀=1.18 μM), MDA-MB-231 (IC₅₀=10.49 μM), MCF-10A (IC₅₀=24.76 μM) cells^[1]. VEGFR2-IN-1 (MCF-7 cells; 48 hours) induces cell cycle arrest at the G1 and S-phases^[1]. VEGFR2-IN-1 (MCF-7 cells) shows the upregulation of pro-apoptotic genes (p53, Bax, caspases-3, caspases-9) and downregulation of antiapoptotic gene (Bcl-2)^[1].

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

VEGFR2-IN-1 (4.2 mg/kg; i.p.; once a day for 7 days) shows anticancer activity with an improvement of hematological, biochemical parameters^[1]. Animal Model: Male Swiss albino mice, 21-28 g (Xenograft model)^[1].

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

398.48

C₂₂H₁₈N₆S

2765224-55-1

C=CCSC1=NN=C(N1/N=C/C2=CNC3=CC=CC=C23)C4=CC5=CC=CC=C5N4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nafie MS, Boraei ATA. Exploration of novel VEGFR2 tyrosine kinase inhibitors via design and synthesis of new alkylated indolyl-triazole Schiff bases for targeting breast cancer. Bioorg Chem. 2022; 122:105708.  [Content Brief]