Name: PX 866
Price: 231.00 USD

- Overview
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    Background
    
    IC50: 0.1-88 nMPX 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].
    
    [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.
- Properties
  - Alternative 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
    
    CAS Number
    
    502632-66-8
    
    Molecular Formula
    
    C29H35NO8
    
    Molecular Weight
    
    525.6
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤25mg/ml in ethanol;14mg/ml in DMSO;25mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only