ZSTK474 is a triazine derivative that acts as an inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms (IC50s = 17, 53, and 6 nM for p110beta, -gamma, and -delta, respectively). It is selective for PI3K, as it has negligible activity against 139 other kinases when tested at 30 µM. ZSTK474 is orally...

ZSTK474 is an inhibitor of PI3K that exhibits anticancer chemotherapeutic, anti-inflammatory, and anti-arthritis activities. ZSTK474 suppresses expression of matrix metalloproteinases (MMPs), VEGF, and HIF-1 , inhibiting migration, invasion, and adhesive capability of prostate cancer cells. ZSTK474 also induces G1...

ZSTK474, a novel s-triazine derivative, binds to the ATP-binding site of Class I phosphatidylinositol 3-kinases (PI3K) and inhibits PI3K activity. ZSTK474 has strong antitumor activities against human cancer xenografts (A549, PC-3 and WiDr) when administered orally to mice. Furthermore, ZSTK474 did not show...

Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol. ZSTK474 inhibits all four PI3K isoforms in an ATP-competitive manner. IC(50) is approximately 37nM. Target: PI3K , Kinase Group: Lipid Kinase , Substrate: Lipid

Description: PI3K Inhibitor ZSTK474 is an orally available, s-triazine derivative, ATP-competitive phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Target: PI3K, Autophagy. Smiles: FC(F)c1nc2ccccc2n1-c1nc(nc(n1)N1CCOCC1)N1CCOCC1. References: Yaguchi S, et al. J Natl Cancer...