• 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.
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