P-7501 PX-866, >99%

Synonyms : [DJM-166] [DJM-2-166] [Sonolisib]

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  • 1 mg
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  • M.W. 525.59
  • C29H35NO8
  • [502632-66-8]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 200 mg/mL; soluble in ethanol at 200 mg/mL; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.

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  • PX-866, a derivative of wortmannin, potently inhibited purified phosphoinositide (PtdIns)-3-kinase (IC50 = 0.1 nM) and PtdIns-3-kinase signaling (IC50 = 20 nM) as assessed by phospho-Ser473-Akt levels in HT-29 colon cancer cells. PX-866 showed antitumor activity in vivo against s.c. A-549 human lung cancer xenografts and OvCar-3 human ovarian cancer in immunodeficient mice. PX-866 also enhanced the antitumor activity of cisplatin against A-549 xenografts and radiation treatment against OvCar-3 xenografts. Ihle, N.T., et al. "Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling." Mol. Cancer Ther. 3: 763-772 (2004).
  • PX-866 appears to inhibit tumor growth by blocking the phosphatidylinositol 3-kinase (PI3K) pathway and cell motility. Howes, A.L., et al. "The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional cultures." Mol. Cancer Ther. 6: 2505-2514 (2007).
  • Hyperglycemia is a side effect of PX-866 treatment. Combination treatment of peroxisome proliferator-activated receptor γ agonist pioglitazone with PX-688 can overcome the increase in blood glucose without affecting antitumor activity caused by PX-866. Ihle, N.T., et al. "Peroxisome proliferator-activated receptor gamma agonist pioglitazone prevents the hyperglycemia caused by phosphatidylinositol 3-kinase pathway inhibition by PX-866 without affecting antitumor activity." Mol. Cancer Ther. 8: 94-100 (2009).
  • PX-866 is a PI3-K inhibitor with selectivity for p110α. It enhanced the antitumor activity of gefitinib against A-549 non-small cell lung cancer (NSCLC) xenografts, giving complete tumor growth control during the early stages of treatment. Ihle, N.T., et al. "The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts." Mol. Cancer Ther. 4: 1349-1357 (2005).
  • STRUCTURE NOTE: Chemical Abstracts Service defines PX-866 as having the "E" configuration for the enamine double bond at the lower left corner of the structure. At least one other vendor's structure for PX-866 has the incorrect "Z" configuration for that double bond.
  • 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.