VEGFR-2-IN-28

VEGFR-2-IN-28 (compound 12c) is a potent VEGFR-2 inhibitor with IC50 value of 0.83 µM. VEGFR-2-IN-28 induces apoptosis and has anticancer activity[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

VEGFR-2:0.83 μM (IC50)

VEGFR-2-IN-28 (compound 12c) (24 hours; MCF-7 cells) has anticancer activity with IC50 value of 16.50 µM[1]. VEGFR-2-IN-28 (compound 12c) (24 hours; MCF-7 cells) prompts pre-G1 apoptosis, cell growth cessation at G2/M phase and induces apoptosis via activation of caspase-3[1]. Apoptosis Analysis[1] Cell Line: MCF-7 cells Concentration: 16.50 µM Incubation Time: 24 hours Result: Induced apoptotic cells resulting in apoptosis percentage 28.41 %. Cell Cycle Analysis[1] Cell Line: MCF-7 cells Concentration: 16.50 µM Incubation Time: 24 hours Result: Increased in the percentage of cells at pre-G1 phase and at G2/M phase to 28.41% and 46.05%, respectively. Immunofluorescence[1] Cell Line: MCF-7 cells Concentration: 16.50 µM Incubation Time: 24 hours Result: Increased in the level of caspase-3.

[1]. Dawood DH, et al. Synthesis and molecular docking study of new pyrazole derivatives as potent anti-breast cancer agents targeting VEGFR-2 kinase. Bioorg Chem. 2020 Aug;101:103916.