(3E)-5-氯-3-[[5-[3-[(六氢-4-甲基-1H-14-二氮杂革-1-基)羰基]苯基]-2-呋喃]亚甲基]-1,3-二氢-2H-吲哚-2-酮

• 常用名: (3E)-5-氯-3-[[5-[3-[(六氢-4-甲基-1H-14-二氮杂革-1-基)羰基]苯基]-2-呋喃]亚甲基]-1,3-二氢-2H-吲哚-2-酮
• 英文名: CX-6258
• CAS号: 1202916-90-2
• 分子量: 461.940
• 密度: 1.3±0.1 g/cm3
• 沸点: 697.8±55.0 °C at 760 mmHg
• 分子式: C₂₆H₂₄ClN₃O₃
• 熔点: N/A
• 闪点: 375.8±31.5 °C

用途

CX-6258是口服活性的Pim 1，2和3激酶抑制剂，IC50为5 nM，25 nM和16 nM。

名称

• 中文名: (3E)-5-氯-3-[[5-[3-[(六氢-4-甲基-1H-14-二氮杂革-1-基)羰基]苯基]-2-呋喃]亚甲基]-1,3-二氢-2H-吲哚-2-酮
• 英文名: (3E)-5-Chloro-3-[(5-{3-[(4-methyl-1,4-diazepan-1-yl)carbonyl]phen yl}-2-furyl)methylene]-1,3-dihydro-2H-indol-2-one

生物活性

• 描述: CX-6258是口服活性的Pim 1,2和3激酶抑制剂,IC50为5 nM,25 nM和16 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]. Mustapha Haddach, Jerome Michaux, Michael K, Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med. Chem. Lett., 2012, 3 (2), pp 135-139

  [2]. Padmanabhan A, Gosc EB, Bieberich CJ. Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cells. J Cell Biochem. 2013 May;114(5):1050-7.

物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 697.8±55.0 °C at 760 mmHg
• 分子式: C₂₆H₂₄ClN₃O₃
• 分子量: 461.940
• 闪点: 375.8±31.5 °C
• 精确质量: 461.150604
• PSA: 69.28000
• LogP: 4.33
• 外观性状: yellow solid
• 蒸汽压: 0.0±2.2 mmHg at 25°C
• 折射率: 1.646
• 储存条件: -20℃

靶点实验

查看更多实验

实验名称：Antitumor activity against human MV411 cells xenografted in nude mouse assessed as tu... 来源：ChEMBL 靶标：MV4-11 External Id：CHEMBL2038848

实验名称：Antitumor activity against human MV411 cells xenografted in po dosed nude mouse asses... 来源：ChEMBL 靶标：MV4-11 External Id：CHEMBL2038849

实验名称：Thermal Shift Assay. Domain start/stop: M626-G740 来源：ChEMBL 靶标：Peregrin External Id：CHEMBL4650107

实验名称：Thermal Shift Assay. Domain: start/stop: M1-L298 来源：ChEMBL 靶标：Cyclin-dependent kinase 2 External Id：CHEMBL5062802

实验名称：Antitumor activity against human MV411 cells xenografted in nude mouse assessed as tu... 来源：ChEMBL 靶标：MV4-11 External Id：CHEMBL2038847

实验名称：Toxicity in human MV411 cells xenografted nude mouse assessed as mortality at 50 to 1... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL2038852

实验名称：Toxicity in human PC3 cells xenografted nude mouse assessed as mortality at 50 to 100... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL2038853

实验名称：Antitumor activity against human PC3 cells xenografted in nude mouse assessed as tumo... 来源：ChEMBL 靶标：PC-3 External Id：CHEMBL2038850

实验名称：Inhibition of Flt3 using EAIYAAPFAKKK as substrate at 0.5 uM by radiometric assay 来源：ChEMBL 靶标：Receptor-type tyrosine-protein kinase FLT3 External Id：CHEMBL2038840

实验名称：Inhibition of human recombinant Pim2 using RSRHSSYPAGT as substrate at 0.5 uM by radi... 来源：ChEMBL 靶标：Serine/threonine-protein kinase pim-2 External Id：CHEMBL2038838

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英文别名

• (E)-5-butyl-2-methyl-hexa-2,5-dien-1-ol
• (3E)-5-Chloro-3-[(5-{3-[(4-methyl-1,4-diazepan-1-yl)carbonyl]phenyl}-2-furyl)methylene]-1,3-dihydro-2H-indol-2-one
• (E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one
• 2-Nonen-1-ol,2-methyl-5-methylene-,(E)
• CX6258
• CX-6258