1876467-74-1

• 常用中文名：BAY-1895344
• 常用英文名：Elimusertib (BAY-1895344) hydrochloride
• CAS号：1876467-74-1
• 分子式：C₂₀H₂₂ClN₇O
• 分子量：411.89
• 相关类别： 信号通路 细胞周期/DNA损伤 ATM/ATR
• 发布时间：2018-05-20 08:00:00
• 更新时间：2026-07-17 19:28:20
• BAY-1895344 是一种有效、可口服、选择性的 ATR 抑制剂,IC50 值为 7 nM。具有抗肿瘤活性。

名称

• 中文名: BAY-1895344
• 英文名: BAY-1895344
• 中文别名: (R)-3-甲基-4-(4-(1-甲基-1H-吡唑-5-基)-8-(1H-吡唑-3-基)-1,7-二氮杂萘-2-基)吗啉; BAY-1895344盐酸盐; (R)-3-甲基-4-[4-(1-甲基-5-吡唑基)-8-(5-吡唑基)-1,7-萘啶-2-基]吗啉; 3-甲基-4-[4-(1-甲基-1H-吡唑-5-基)-8-(1H-吡唑-3-基)-1,7-萘啶-2-基]吗啉; 2-[(3R)-3-甲基-4-吗啉基]-4-(1-甲基-1H-吡唑-5-基)-8-(1H-吡唑-3-基)-1,7-萘啶
• 英文别名: Elimusertib free base; Elimusertib, 10 mM in DMSO; (R)-3-Methyl-4-(4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-3-yl)-1,7-naphthyridin-2-yl)morpholine , Elimusertib; 1,7-Naphthyridine, 2-[(3R)-3-methyl-4-morpholinyl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-3-yl); 3-methyl-4-(4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-3-yl)-1,7-naphthyridin-2-yl)morpholine; BAY-1895344 HCl(Elimusertib); BAY-1895344 diHCl; BAY1895344;BAY 1895344;D; MFCD31561442; D1213; BAY1895344;BAY 1895344;BAY-1895344; (R)-3-Methyl-4-[4-(1-methyl-5-pyrazolyl)-8-(5-pyrazolyl)-1,7-naphthyridin-2-yl]morpholine; BAY 1895344 (BAY-1895344); (R)-3-methyl-4-(4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-3-yl)-1,7-naphthyridin-2-yl)morpholine; Elimusertib; (R)-3-methyl-4-(4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridin-2-yl)morpholine; Elimusertib (BAY1895344)

物化性质

• 分子式: C₂₀H₂₂ClN₇O
• 分子量: 411.89
• 外观性状: 粉末
• 储存条件: -20℃

生物活性

• 描述: BAY-1895344 是一种有效、可口服、选择性的 ATR 抑制剂,IC50 值为 7 nM。具有抗肿瘤活性。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> ATM/ATR
  信号通路 >> PI3K/Akt/mTOR 信号通路 >> ATM/ATR
• 靶点:

  ATR:7 nM (IC50)

• 体外研究: BAY-1895344有效抑制广谱人肿瘤细胞系的增殖,中位IC50为78 nM [1]。 BAY-1895344有效抑制羟基脲诱导的H2AX磷酸化(IC50,36 nM)[1]。
• 体内研究: BAY-1895344在卵巢癌和结肠直肠癌的各种异种移植模型中显示出有效的抗肿瘤功效,并且在套细胞淋巴瘤模型中导致完全肿瘤缓解[2]。
• 参考文献:

  [1]. Ulrich T. Luecking, et al. Abstract 983: Identification of potent, highly selective and orally available ATR inhibitor BAY 1895344 with favorable PK properties and promising efficacy in monotherapy and combination in preclinical tumor models. Cancer Research. July 2017 Volume 77, Issue 13 Supplement.

  [2]. Antje Margret Wengner, et al. Abstract 836: ATR inhibitor BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride in preclinical tumor models. Cancer Research. July 2017 Volume 77, Issue 13 Supplement

安全

• 危害码 (欧洲): N