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Catalog # CD0279

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(1E,4S,4aR,5R,6aS,9aR)- 5-(Acetyloxy)-1-[(di-2-propen-1-ylamino)methylene]-4,4a,5,6,6a,8,9,9a-octahydro-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethylcyclopenta[5,6]naphtho[1,2-c]pyran-2,7,10(1H)-trione


Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity: 98% by HPLC. CAS# 502632-66-8. Solubility: DMSO, MeOH. Molecular Formula: C29H35NO8. Molecular Weight: 525.6.



Biologically stable, semisynthetic derivative of wortmannin. PX-866 is more potent that its parent compound, wortmannin. PX-866 is a PI3-K inhibitor with selectivity for p110α.


Administered to mice at 10 mg/kg inhibited phospho-Ser473-Akt in HT-29 colon tumor xenografts up to 80% with recovery taking >48 hours after p.o. administration but more rapidly after i.v. or i.p. administration. PX-866 exhibited in vivo antitumor activity against s.c. OvCar-3 human ovarian cancer and A-549 human lung cancer xenografts in immunodefficient mice with log cell kills up to 1.2.


A major toxicity of PX-866 administration was hyperglycemia with decreased glucose tolerance, which was reversed upon cessation of treatment. The decreased glucose tolerance caused by PX-866 was insensitive to the AMP-activated protein kinase inhibitor metformin but reversed by insulin and by the peroxisome proliferator-activated receptor-γ activator pioglitazone.


PX-866 increases the antitumor effects of cisplatin and radiation treatment.


References: 1. Ihle, N. T. et al Mol. Canc. Ther. 2009, 8, 94; 2. Howes, A. L. et al Mol. Canc. Ther. 2007, 6, 2505; 3. Ihle, N. T. et al Mol. Canc. Ther. 2005, 4, 1349; 4. Ihle, N. T. et al Mol. Canc. Ther. 2004, 3, 763.





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Caution Not fully tested. For research use only. Not for human use.

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