ZSTK474, Free Base **

产品名称：ZSTK474, Free Base
产品货号：LC  Z-1066
产品规格：1 G
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.  Yaguchi, S., et al.  "Antitumor Activity of ZSTK474, a New Phosphatidylinositol 3-Kinase Inhibitor."  J. Natl. Cancer Inst. 98:  545-556 (2006).
The Class I PI3K inhibitory activity of ZSTK474 is not isoform-specific within the class -- it is an ATP-competitive inhibitor of all four Class I PI3K isoforms.  However, ZSTK474 inhibits PI3Kδ most potently, with a Ki of 1.8 nM, while it inhibits the α, β and γ isoforms at slightly higher concentrations (6.7 nM, 10.4 nM and 11.7 nM, respectively).  Kong, D. and Yamori, T.  "ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms."  Cancer Sci. 98:  1638-1642 (2007).
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.
ZSTK474 is also less toxic than LY 294002 and wortmannin in animal model tests.  Yaguchi, S., et al., op. cit.
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 20 mg/mL; soluble in ethanol at 2.5 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 1-5 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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