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 抑制 HepG2、MCF-7、A549、HT-29、PC3 和 WI-38 细胞增殖，其 IC50 分别为 7.28、6.72、6.66、8.51、14.5 和 30 μM [1]。在 HT-29 细胞中，VEGFR-2-IN-58 (8.51 μM, 24 h) 除了诱导凋亡，还导致 G2/M 期细胞生长抑制 [1]。同时，VEGFR-2-IN-58 (0.85, 4.26 μM, 48 h) 在 HT-29 细胞中明显抑制伤口愈合 [1]。