VEGFR-2-IN-58 (Compound 7b) is a VEGFR-2 inhibitor with an IC50 of 42.5 nM. It shows selective cytotoxicity against cancer cells, induces cell cycle arrest at the G2/M phase, and triggers apoptosis by increasing BAX expression and decreasing Bcl2 expression. Additionally, VEGFR-2-IN-58 hampers cancer cell wound closure.

VEGFR2:42.5 nM

VEGFR-2-IN-58 inhibits the proliferation of HepG2, MCF-7, A549, HT-29, PC3, and WI-38 cells with IC₅₀ values of 7.28, 6.72, 6.66, 8.51, 14.5, and 30 μM, respectively [1]. In HT-29 cell lines, VEGFR-2-IN-58 (8.51 μM, 24 h) not only induces apoptosis but also exhibits G2/M phase cell growth inhibition [1]. Additionally, VEGFR-2-IN-58 (0.85, 4.26 μM, 48 h) significantly impedes wound healing in HT-29 cells [1].