1820565-69-2

• 常用中文名：PIM-447二盐酸盐
• 常用英文名：PIM-447 dihydrochloride
• CAS号：1820565-69-2
• 分子式：C₂₄H₂₅Cl₂F₃N₄O
• 分子量：513.383
• 相关类别： 信号通路 JAK/STAT信号通路 皮姆
• 发布时间：2018-04-02 09:34:34
• 更新时间：2024-04-05 19:33:07
• PIM447是一个新颖的pan-PIM抑制剂。

名称

• 中文名: PIM-447二盐酸盐
• 英文名: N-{4-[(1R,3S,5S)-3-Amino-5-methylcyclohexyl]-3-pyridinyl}-6-(2,6-difluorophenyl)-5-fluoro-2-pyridinecarboxamide dihydrochloride
• 英文别名: 2-Pyridinecarboxamide, N-[4-[(1R,3S,5S)-3-amino-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoro-, hydrochloride (1:2); N-{4-[(1R,3S,5S)-3-Amino-5-methylcyclohexyl]-3-pyridinyl}-6-(2,6-difluorophenyl)-5-fluoro-2-pyridinecarboxamide dihydrochloride; PIM-447 dihydrochloride; PIM-447 (dihydrochloride)

物化性质

• 分子式: C₂₄H₂₅Cl₂F₃N₄O
• 分子量: 513.383
• 精确质量: 512.135742
• 储存条件: 2-8℃

生物活性

• 描述: PIM447是泛PIM激酶抑制剂,对PIM1,PIM2,PIM3的 Ki 分别为6,18,9 nM。
• 相关类别:
  信号通路 >> JAK/STAT信号通路 >> 皮姆
  研究领域 >> 癌症
• 参考文献:

  [1]. Paíno T et al. The novel pan-PIM kinase inhibitor, PIM447, displays dual anti-myeloma and bone protective effects, and potently synergizes with current standards of care. Clin Cancer Res. 2016 Jul 20.

  [2]. Burger MT et al. Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies. J Med Chem. 2015 Nov 12;58(21):8373-86.

  [3]. Peters TL et al. Control of translational activation by PIM kinase in activated B-cell diffuse large B-cell lymphoma confers sensitivity to inhibition by PIM447.Oncotarget. 2016 Aug 20