502632-66-8

• 常用中文名：Sonolisib
• 常用英文名：PX-866
• CAS号：502632-66-8
• 分子式：C₂₉H₃₅NO₈
• 分子量：525.590
• 相关类别： 信号通路 PI3K/Akt/mTOR 信号通路 PI3K
• 发布时间：2017-08-02 12:28:55
• 更新时间：2024-01-04 22:20:23
• 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。

名称

• 英文名: [(3aR,6E,9S,9aR,10R,11aS)-6-[[bis(prop-2-enyl)amino]methylidene]-5-hydroxy-9-(methoxymethyl)-9a,11a-dimethyl-1,4,7-trioxo-2,3,3a,9,10,11-hexahydroindeno[4,5-h]isochromen-10-yl] acetate
• 英文别名: Cyclopenta[5,6]naphtho[1,2-c]pyran-2,7,10(1H)-trione, 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-, (1E,4S,4aR,5R,6aS,9aR)-; PX-866; (1E,4S,4aR,5R,6aS,9aR)-1-[(diprop-2-en-1-ylamino)methylidene]-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,7,10-trioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; DJM-2-166; (1E,4S,4aR,5R,6aS,9aR)-1-[(Diallylamino)methylene]-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-2,7,10-trioxo-1,2,4,4a,5,6,6a,7,8,9,9a,10-dodecahydroindeno[4,5-h]isochromen-5-yl acetate; DJM-166; Sonolisib

物化性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 651.4±55.0 °C at 760 mmHg
• 分子式: C₂₉H₃₅NO₈
• 分子量: 525.590
• 闪点: 347.7±31.5 °C
• 精确质量: 525.236267
• PSA: 119.44000
• LogP: 2.37
• 蒸汽压: 0.0±4.4 mmHg at 25°C
• 折射率: 1.586
• 储存条件: -20°C，干燥，密封

生物活性

• 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。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> PI3K/Akt/mTOR 信号通路 >> PI3K
• 靶点:

  p110α:0.1 nM (IC50)

  p110δ:2.9 nM (IC50)

  p120γ:1 nM (IC50)

• 体外研究: Sonolisib(PX-866)抑制二级信使磷脂酰肌醇-3,4,5-三磷酸(PIP3)的产生和PI3K/AKT信号通路的激活,这可能抑制肿瘤细胞生长和易感肿瘤细胞群的存活[3]。
• 参考文献:

  [1]. Ihle NT, et al. The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growthfactor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts. Mol Cancer Ther. 2005 Sep;4(9):1349-57.

  [2]. Bowles DW, et al. A Randomized, Phase II Trial of Cetuximab With or Without PX-866, an Irreversible Oral Phosphatidylinositol 3-Kinase Inhibitor, in Patients With Metastatic Colorectal Carcinoma. Clin Colorectal Cancer. 2016 Dec;15(4):337-344.e2.

  [3]. Sonolisib