1101810-02-9

• 常用中文名：AZD 3147,双重MTORC1和2抑制剂
• 常用英文名：AZD 3147
• CAS号：1101810-02-9
• 分子式：C₂₄H₃₁N₅O₄S₂
• 分子量：517.664
• 相关类别： 信号通路 PI3K/Akt/mTOR 信号通路 mTOR
• 发布时间：2018-01-27 17:44:38
• 更新时间：2026-07-16 10:57:34
• AZD3147是mTORC1和mTORC2的有效、口服活性、选择性双重抑制剂,IC50值为1.5nM。AZD3147对PI3K也有选择性作用[1]。

名称

• 中文名: AZD 3147,双重MTORC1和2抑制剂
• 英文名: AZD3147
• 中文别名: (S)-1-(4-(4-(1-(环丙基磺酰基)环丙基)-6-(3-甲基吗啉-4-基)嘧啶-2-基)苯基)-3-(2-羟基乙基)硫脲
• 英文别名: Thiourea, N-[4-[4-[1-(cyclopropylsulfonyl)cyclopropyl]-6-[(3S)-3-methyl-4-morpholinyl]-2-pyrimidinyl]phenyl]-N'-(2-hydroxyethyl); (S)-1-(4-(4-(1-(cyclopropylsulfonyl)cyclopropyl)-6-(3-methylmorpholino)pyrimidin-2-yl)phenyl)-3-(2-hydroxyethyl)thiourea; AZ-12600000; N-[4-[4-[1-(cyclopropylsulfonyl)cyclopropyl]-6-[(3S)-3-methyl-4-morpholinyl]-2-pyrimidinyl]phenyl]-N'-(2-hydroxyethyl)-thiourea; 1-(4-{4-[1-(Cyclopropylsulfonyl)cyclopropyl]-6-[(3S)-3-methyl-4-morpholinyl]-2-pyrimidinyl}phenyl)-3-(2-hydroxyethyl)thiourea; (S)-1-(4-(4-(1-(Cyclopropylsulfonyl)cyclopropyl)-6-(3-methylmorpholin-4-yl)-pyrimidin-2-yl)phenyl)-3-(2-hydroxyethyl)thiourea; N-[4-[4-[1-(Cyclopropylsulfonyl)cyclopropyl]-6-[(3S)-3-methyl-4-morpholinyl]-2-pyrimidinyl]phenyl]-N'-(2-hydroxyethyl)thiourea; AZD 3147, 10 mM in DMSO; 1-[4-[4-(1-cyclopropylsulfonylcyclopropyl)-6-[(3S)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]-3-(2-hydroxyethyl)thiourea

物化性质

• 密度: 1.5±0.1 g/cm3
• 沸点: 696.7±65.0 °C at 760 mmHg
• 分子式: C₂₄H₃₁N₅O₄S₂
• 分子量: 517.664
• 闪点: 375.2±34.3 °C
• 精确质量: 517.181763
• LogP: -0.58
• 蒸汽压: 0.0±2.3 mmHg at 25°C
• 折射率: 1.689

生物活性

• 描述: AZD3147是mTORC1和mTORC2的有效、口服活性、选择性双重抑制剂,IC50值为1.5nM。AZD3147对PI3K也有选择性作用[1]。
• 相关类别:
  信号通路 >> PI3K/Akt/mTOR 信号通路 >> mTOR
  研究领域 >> 癌症
• 靶点:

  mTORC1

  mTORC2

• 体外研究: AZD3147(0-50nM,1h)在NIH3T3细胞中浓度高于1.5nM时可减轻成纤维细胞生长因子(FGF)介导的纤毛延伸[2]。AZD3147抑制神经母细胞瘤细胞系Kelly和IMR-32的细胞活力,IC50值分别为0.88nM和662.4nM[3]。
• 体内研究: AZD3147的药代动力学参数[1]。小鼠和狗的参数CL(mL/min/kg)78 16 Vss(L/kg)2.3 2.2 t1/2(h)0.9 1.9 F%61 73
• 参考文献:

  [1]. Kurt G Pike, et al. Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2. J Med Chem. 2015 Mar 12;58(5):2326-49.

  [2]. Michaela Kunova Bosakova, et al. Regulation of ciliary function by fibroblast growth factor signaling identifies FGFR3-related disorders achondroplasia and thanatophoric dysplasia as ciliopathies. Hum Mol Genet. 2018 Mar 15;27(6):1093-1105.

  [3]. Rebecca Waetzig, et al. Comparing mTOR inhibitor Rapamycin with Torin-2 within the RIST molecular-targeted regimen in neuroblastoma cells. Int J Med Sci. 2021 Jan 1;18(1):137-149.