| Identification | Back Directory | [Name]
PX-13-17OH | [CAS]
884539-95-1 | [Synonyms]
PX-13-17OH
Cyclopenta[5,6]naphtho[1,2-c]pyran-2,10(1H,4H)-dione, 5-(acetyloxy)-1-[[[3-(dimethylamino)propyl]methylamino]methylene]-4a,5,6,6a,7,8,9,9a-octahydro-7,11-dihydroxy-4-(methoxymethyl)-4a,6a-dimethyl-, (1E,4S,4aR,5R,6aS,7S,9aR)- | [Molecular Formula]
C29H42N2O8 | [MOL File]
884539-95-1.mol | [Molecular Weight]
546.65 |
| Chemical Properties | Back Directory | [Boiling point ]
662.308±55.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.283±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A crystalline solid | [pka]
6.198±0.70(predicted) |
| Hazard Information | Back Directory | [Description]
PX-13-17OH is a PI3K inhibitor | [Uses]
PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg. | [References]
[1] Zask, et al. Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: Potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy. J. Med. Chem. 51(5), 1319-1323 (2008). |
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