ZSTK474/ZSTK-474/

溶解度:Soluble in DMSO at 20 mg/mL; soluble in ethanol at 2.5 mg/mL with warming

储存条件:Storage at -20C 2 years

生物活性

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 significant toxicity at the doses tested.

参考文献

1. Yaguchi, S., et al. "Antitumor Activity of ZSTK474, a New Phosphatidylinositol 3-Kinase Inhibitor." J. Natl. Cancer Inst. 98: 545-556 (2006).

2. Kong, D. and Yamori, T. "ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol

3 kinase isoforms." Cancer Sci. 98: 1638-1642 (2007). 3. ZSTK474 is a far more potent Class I PI3K inhibitor than LY294002, by a factor of 30-fold or more, and it is far more stable than wortmannin. Kong, D. and Yamori, T., ibid.