5-chloro-2-N-[2-methoxy-4-[4-[(4-methylpiperazin-1-yl)methyl]triazol-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine

• 常用名: 5-chloro-2-N-[2-methoxy-4-[4-[(4-methylpiperazin-1-yl)methyl]triazol-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine
• 英文名: WY-135
• CAS号: 2163060-83-9
• 分子量: 612.15
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₈H₃₄ClN₉O₃S
• 熔点: N/A
• 闪点: N/A

用途

WY-135是ALK (IC50=1.4 nM) 和 ROS1 (IC50=1.1 nM) 的双抑制剂。

名称

• 中文名: WY-135
• 英文名: WY-135

生物活性

• 描述: WY-135是ALK (IC50=1.4 nM) 和 ROS1 (IC50=1.1 nM) 的双抑制剂。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 蛋白酪氨酸激酶 >> ROS
  信号通路 >> 蛋白酪氨酸激酶 >> ALK
• 靶点实验:

  IC50: 1.4 nM (ALK), 1.1 nM (ROS1)[1]

• 参考文献:

  [1]. Wang Y, et al. Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R. Eur J Med Chem. 2018 Jan 1;143:123-136.

物理化学性质

• 分子式: C₂₈H₃₄ClN₉O₃S
• 分子量: 612.15
• 储存条件: 2-8°C，密封，干燥

靶点实验

查看更多实验

实验名称：Inhibition of recombinant human N-terminal GST-tagged c-MET cytoplasmic domain (956 t... 来源：ChEMBL 靶标：Hepatocyte growth factor receptor External Id：CHEMBL4136450

实验名称：Inhibition of recombinant human N-terminal GST-tagged EGFR cytoplasmic domain (669 to... 来源：ChEMBL 靶标：Epidermal growth factor receptor External Id：CHEMBL4136451

实验名称：Downregulation of ALK protein expression in human KARPAS299 cells after 6 hrs by West... 来源：ChEMBL 靶标：KARPAS-299 External Id：CHEMBL4136464

实验名称：Downregulation of ROS1 protein expression in human HCC78 cells at 100 nM after 6 hrs ... 来源：ChEMBL 靶标：HCC78 External Id：CHEMBL4136465

实验名称：Inhibition of ALK phosphorylation in human KARPAS299 cells after 6 hrs by Western blo... 来源：ChEMBL 靶标：ALK tyrosine kinase receptor External Id：CHEMBL4136463

实验名称：Induction of apoptosis in human KARPAS299 cells harboring NPM-ALK after 24 hrs by acr... 来源：ChEMBL 靶标：KARPAS-299 External Id：CHEMBL4136460

实验名称：Induction of apoptosis in human HCC78 cells harboring SLC34A2-ROS1 after 24 hrs by ac... 来源：ChEMBL 靶标：HCC78 External Id：CHEMBL4136461

实验名称：Potency index, ratio of ceritinib IC50 to compound IC50 for recombinant human N-termi... 来源：ChEMBL 靶标：ALK tyrosine kinase receptor External Id：CHEMBL4136458

实验名称：Potency index, ratio of ceritinib IC50 to compound IC50 for recombinant human N-termi... 来源：ChEMBL 靶标：ALK tyrosine kinase receptor External Id：CHEMBL4136459

实验名称：Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 h... 来源：ChEMBL 靶标：KARPAS-299 External Id：CHEMBL4136441

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