CHMFL-ABL/KIT-155

• 常用名: CHMFL-ABL/KIT-155
• 英文名: CHMFL-ABL/KIT-155
• CAS号: 2081093-21-0
• 分子量: 609.68
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₃H₃₈F₃N₅O₃
• 熔点: N/A
• 闪点: N/A

CHMFL-ABL/KIT-155用途

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) 是一种高效的,具有口服活性的 type II ABL/c-KIT 双激酶抑制剂 (IC50 分别为 46 nM 和 75 nM),对 BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM), PDGFRβ (IC50=80 nM) 激酶也具有明显的抑制活性。CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) 阻止细胞周期进展和诱导细胞凋亡。

CHMFL-ABL/KIT-155名称

• 英文名: CHMFL-ABL/KIT-155

CHMFL-ABL/KIT-155生物活性

• 描述: CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) 是一种高效的,具有口服活性的 type II ABL/c-KIT 双激酶抑制剂 (IC50 分别为 46 nM 和 75 nM),对 BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM), PDGFRβ (IC50=80 nM) 激酶也具有明显的抑制活性。CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) 阻止细胞周期进展和诱导细胞凋亡。
• 相关类别:
  信号通路 >> 细胞凋亡 >> 细胞凋亡
  研究领域 >> 癌症
  信号通路 >> 蛋白酪氨酸激酶 >> BCR-ABL
  信号通路 >> 蛋白酪氨酸激酶 >> c-Kit
• 靶点实验:

  IC50: 46 nM (type II ABL), 75 nM (c-KIT), 81 nM (BLK), 227 nM (CSF1R), 116 nM (DDR1), 325 nM (DDR2), 12 nM (LCK), 80 nM (PDGFRβ)[1]

• 体外研究: chmfl-abl/kit-155(chmfl-abl-kit-155)在诸如k562(gi50:0.027μm)、meg-01(gi50:0.02μm)和ku812(gi50:0.056μm)等BCR-abl依赖性CML癌细胞系中表现出抗增殖活性。它也能有效抑制c-kit依赖的gists癌细胞株的生长,包括gist-T1(gi50:0.023μm)、gist-882(gi50:0.095μm),但不抑制c-kit独立的gist-48b(gi50:3.96μm)[1]。
• 体内研究: chmfl-abl/kit-155(chmfl-abl-kit-155)(25-100 mg/kg；p.o.；每天一次,持续28天)显示,在携带已建立的K562异种肿瘤移植物的雌性nu/nu小鼠中,剂量依赖性肿瘤进展抑制没有明显毒性[1]。
• 参考文献:

  [1]. Wang Q, et al. Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. J Med Chem. 2017 Jan 12;60(1):273-289.

CHMFL-ABL/KIT-155物理化学性质

• 分子式: C₃₃H₃₈F₃N₅O₃
• 分子量: 609.68

CHMFL-ABL/KIT-155靶点实验

查看更多实验

实验名称：Inhibition of c-KIT autophosphorylation at Y719 in human GIST882 cells at 0.01 to 3 u... 来源：ChEMBL 靶标：Mast/stem cell growth factor receptor Kit External Id：CHEMBL3879045

实验名称：Inhibition of c-KIT autophosphorylation at Y823 in human GIST882 cells at 0.01 to 3 u... 来源：ChEMBL 靶标：Mast/stem cell growth factor receptor Kit External Id：CHEMBL3879046

实验名称：Inhibition of c-KIT mediated signaling pathways assessed as reduction in AKT phosphor... 来源：ChEMBL 靶标：Mast/stem cell growth factor receptor Kit External Id：CHEMBL3879047

实验名称：Inhibition of c-KIT mediated signaling pathways assessed as reduction in Stat3/5 phos... 来源：ChEMBL 靶标：Mast/stem cell growth factor receptor Kit External Id：CHEMBL3879048

实验名称：Inhibition of c-KIT autophosphorylation at Y703 in human GISTT1 cells at 0.03 to 10 u... 来源：ChEMBL 靶标：Mast/stem cell growth factor receptor Kit External Id：CHEMBL3879041

实验名称：Inhibition of c-KIT autophosphorylation at Y719 in human GISTT1 cells at 0.03 to 10 u... 来源：ChEMBL 靶标：Mast/stem cell growth factor receptor Kit External Id：CHEMBL3879042

实验名称：Inhibition of c-KIT autophosphorylation at Y823 in human GISTT1 cells at 0.03 to 10 u... 来源：ChEMBL 靶标：Mast/stem cell growth factor receptor Kit External Id：CHEMBL3879043

实验名称：Inhibition of c-KIT autophosphorylation at Y703 in human GIST882 cells at 0.01 to 3 u... 来源：ChEMBL 靶标：Mast/stem cell growth factor receptor Kit External Id：CHEMBL3879044

实验名称：Inhibition of c-KIT mediated signaling pathways assessed as reduction in ERK1/2 phosp... 来源：ChEMBL 靶标：Mast/stem cell growth factor receptor Kit External Id：CHEMBL3879053

实验名称：Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6K phosphor... 来源：ChEMBL 靶标：Mast/stem cell growth factor receptor Kit External Id：CHEMBL3879054

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