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.
Solubility:Soluble in DMSO at 200mg/ml; soluble in ethanol at 200mg/ml; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20uM; buffers, serum, or other additives may increase or decrease the aqueous solubility.
Melting Point:102.5-105ºC
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months after receipt at -20°C. Reconstitute with sterile buffer. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.