ZSTK474

ZSTK474 is an orally available, s-triazine derivative and ATP-competitive inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms, developed as a potential anticancer agent. It inhibits all four PI3K isoforms, thereby blocking the activation of the PI3K/AKT signaling pathway, which results in inhibition of tumor cell growth and survival. Unlike some other agents, it induces strong G0/G1 cell cycle arrest rather than apoptosis in tumor cells. ZSTK474 also exhibits potent antiangiogenic activity by inhibiting HIF-1α expression and VEGF production, as well as blocking VEGF-induced migration and tube formation in endothelial cells. The drug has demonstrated strong antitumor activity against human cancer xenografts with low toxicity to critical organs and has shown efficacy in preclinical models of rheumatoid arthritis through inhibition of T cell and fibroblast-like synoviocyte functions[1][2][3][4][5][6][8].

Other names

PI3K inhibitor ZSTK474PI-3K inhibitor ZSTK474PI 3K inhibitor ZSTK474