PX-866 ([(3aR,6E,9S,9aR,10R,11aS)-6-[[bis(prop-2-enyl)amino]methylidene]-5-hydroxy-9-(methoxymethyl)-9a,11a-dimethyl-1,4,7-trioxo-2,3,3a,9,10,11-hexahydroindeno[4,5-h]isochromen-10-yl] acetate, DJM-166, DJM-2-166)

PX-866, a derivative of wortmannin, potently inhibited purified phosphoinositide (PtdIns)-3-kinase (IC50=0.1nM) and PtdIns-3-kinase signaling (IC50=20nM) 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.\n\nSolubility:\nSoluble in DMSO.\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

P9394-50

Size

5mg

Form

Supplied as a powder.

Purity

~99%

References

1. 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). 2. 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). 3. 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). 4. 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).