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化学性质:
规格 | 1mg 5mg 10mg |
CAS | 502632-66-8 |
别名 | N/A |
化学名 | (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 |
分子式 | C29H35NO8 |
分子量 | 525.6 |
溶解度 | ≤25mg/ml in ethanol;14mg/ml in DMSO;25mg/ml in dimethyl formamide |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
IC50: 0.1-88 nM
PX 866 is a PI3K inhibitor.
Phosphoinositide (PtdIns)-3-kinases can phosphorylate membrane PtdIns and there are 8 mammalian PtdIns-3-kinases that are divided into three main classes based on its sequence homology and substrate preference.
In vitro: In previous study, PX 866 was identified to be able to inhibit purified PtdIns-3-kinase and PtdIns-3-kinase signaling that was measured by phospho-Ser473-Akt levels in HT-29 colon cancer cells [1].
In vivo: Animal study found that PX-866 treatment at 10 mg/kg to mice could inhibit phospho-Ser473-Akt in HT-29 colon tumor xenografts up to 80% with recovery taking over 48 hours after oral administration but more rapidly after iv or ip route. In addition, PX-866 had in-vivo antitumor activity against s.c. OvCar-3 human ovarian cancer and A-549 human lung cancer xenografts in immunodeficient mice. Moreove, PX-866 could also increase the antitumor activity of cisplatin against A-549 xenografts and radiation treatment against OvCar-3 xenografts [1].
Clinical trial: In a previous study, PX-866 was administered at 4–8 mg daily with docetaxel 75 mg/m2 every 21 days, and the results showed that the treatment with PX-866 and docetaxel was well tolerated, without evidence of overlapping/cumulative toxicity [2].
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原创作者:上海莼试生物技术有限公司
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