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P-7501 PX-866, >99%

[DJM-166] [DJM-2-166] [DJM 166] [DJM166] [DJM 2-166]

M.W. 525.59

C29H35NO8

[502632-66-8]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO.  Disposal:  A

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View the MSDS for this product

• 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.