Sonolisib
Cat. No.:YN420312
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. |
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)"}] |
In Vitro: | |
In Vivo: | |
Clinical Trial: | |
Solvent & Solubility: |
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)