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PX 866
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PX 866图片
CAS NO:502632-66-8
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
PX 866 (PX-866) 是一种改进的 Wortmannin 类似物，是一种口服的、不可逆的、泛异构体 PI3K 抑制剂 (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110) .抗肿瘤活性。
Cas No.502632-66-8
别名PX-866
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
Canonical SMILESO=C(/C1=C\N(CC=C)CC=C)O[C@H](COC)[C@@]2(C)C1=C(O)C(C3=C2[C@H](OC(C)=O)C[C@@]4(C)[C@@]3([H])CCC4=O)=O
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℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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].

References:
[1] N. T. Ihle, R. Williams, S. Chow, et al. Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling. Molecular Cancer Therapeutics 3(7), 763-772 (2004).
[2] Bowles DW, Ma WW, Senzer N, Brahmer JR, Adjei AA, Davies M, Lazar AJ, Vo A, Peterson S, Walker L, Hausman D, Rudin CM, Jimeno A. 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.