Z-1066 ZSTK474, Free Base, >99%

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  • M.W. 417.41
  • C19H21F2N7O2
  • [475110-96-4]

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.

  • 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.
  • Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.