PX-866
PX-866 is a wortmannin analog that inhibits PI3K, exhibiting anticancer chemotherapeutic and anti-angiogenic activities. PX-866 is currently in clinical trials as a standalone or combination therapy in the treatment of advanced solid tumors. PX-866 inhibits invasion and angiogenesis and induces autophagy in glioblastoma cells. In animal models of cancer, PX-866 inhibits tumor growth and increases survival time. PX-866 also inhibits motility of cancer cells.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18955665
| Cas No. |
502632-66-8 |
|---|---|
| Purity |
≥98% |
| Formula |
C29H35NO8 |
| Formula Wt. |
525.59 |
| Chemical Name |
(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-dimethyl-cyclopenta[5,6]naphtho[1,2-c]pyran-2,7,10(1H)-trione |
| IUPAC Name |
[(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 |
| Synonym |
Sonolisib |
| Melting Point |
102°C-107°C |
| Solubility |
Methanol , DMSO, Ethyl acetate, Ethanol |
| Appearance |
Orange Powder |
Bowles DW, Ma WW, Senzer N, et al. A multicenter phase 1 study of PX-866 in combination with docetaxel in patients with advanced solid tumours. Br J Cancer. 2013 Sep 3;109(5):1085-92. PMID: 23942080.
Koul D, Shen R, Kim YW, et al. Cellular and in vivo activity of a novel PI3K inhibitor, PX-866, against human glioblastoma. Neuro Oncol. 2010 Jun;12(6):559-69. PMID: 20156803.
Howes AL, Chiang GG, Lang ES, 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. 2007 Sep;6(9):2505-14. PMID: 17766839.
