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Sonolisib

Cat. No.:YN420312

  • CAS No. :502632-66-8

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    • 产品名称: Sonolisib
      CAS No.: 502632-66-8
      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
      Synonyms:PX-866
      分子量:525.59
      分子式:C₂₉H₃₅NO₈
      SMILES:O=C1C([C@@](CC2)([H])[C@@]3(C)C2=O)=C([C@H](OC(C)=O)C3)[C@]4(C)C(/C(C(O[C@@H]4COC)=O)=C\N(CC=C)CC=C)=C1O
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: Sonolisib (PX-866),一种改良的 Wortmannin 类似物,是一种可口服的,不可逆的,泛亚型的PI3K抑制剂 (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ))。PX-866 具有出抗肿瘤活性。
      IC50和靶点: [{name:"p110α:0.1 nM (IC50)"},{name: "p110δ:2.9 nM (IC50)"},{name: "p120γ:1 nM (IC50)"}]
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    • Ihle, N.T., Williams, R., Chow, S., et al.Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signalingMol. Cancer Ther.3(7),763-772(2004)

      Zask, A., Kaplan, J., Toral-Barza, L., et al.Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: Potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacyJ. Med. Chem.51(5),1319-1323(2008)

      Ihle, N.T., Paine-Murrieta, G., Berggren, M.I., et al.The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenograftsMol. Cancer Ther.4(9),1349-1357(2005)

      Howes, A.L., Chiang, G.G., Lang, E.S., et al.The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional culturesMol. Cancer Ther.6(9),2505-2514(2007)

      Hong, D.S., Bowles, D.W., Falchook, G.S., et al.A Multicenter phase I trial of PX-866, an oral irreversible phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumorsClin. Cancer Res.18(15),4173-4182(2012)

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