FGFR-IN-8

• 常用名: FGFR-IN-8
• 英文名: FGFR-IN-8
• CAS号: 2640217-64-5
• 分子量: 584.50
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₇H₃₁Cl₂N₉O₂
• 熔点: N/A
• 闪点: N/A

FGFR-IN-8用途

FGFR-IN-8(化合物17a)是一种针对野生型和突变型FGFR的高效口服活性panFGFR抑制剂。FGFR-IN-8对FGFR1、V564F-FGFR2、N549H-FGFR3、V555M-FGFR 3、FGFR3和FGFR4的IC50值分别为＜0.5、189.1、＜0.5、＜22.6、＜1.5和7.30 nM。GFR-IN-8诱导癌细胞凋亡并显示抗癌活性[1]。

FGFR-IN-8名称

• 英文名: FGFR-IN-8

FGFR-IN-8生物活性

• 描述: FGFR-IN-8(化合物17a)是一种针对野生型和突变型FGFR的高效口服活性panFGFR抑制剂。FGFR-IN-8对FGFR1、V564F-FGFR2、N549H-FGFR3、V555M-FGFR 3、FGFR3和FGFR4的IC50值分别为＜0.5、189.1、＜0.5、＜22.6、＜1.5和7.30 nM。GFR-IN-8诱导癌细胞凋亡并显示抗癌活性[1]。
• 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 >> FGFR
• 靶点实验:

  FGFR1:<0.5 nM (IC50)

  V564F-FGFR2:189.1 nM (IC50)

  N549H-FGFR2:<0.5 nM (IC50)

  V555M-FGFR3:22.6 nM (IC50)

  FGFR3:<0.5 nM (IC50)

  FGFR4:7.30 nM (IC50)

  V561M-FGFR1:262.5 nM (IC50)

  K650E-FGFR3:<0.5 nM (IC50)

  K650M-FGFR3:4.8 nM (IC50)

• 参考文献:

  [1]. Ryu S, et al. Identification of Pyridinyltriazine Derivatives as Potent panFGFR Inhibitors against Gatekeeper Mutants for Overcoming Drug Resistance. J Med Chem. 2022 Apr 28;65(8):6017-6038.

FGFR-IN-8物理化学性质

• 分子式: C₂₇H₃₁Cl₂N₉O₂
• 分子量: 584.50

FGFR-IN-8靶点实验

查看更多实验

实验名称：Anti-migratory activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant... 来源：ChEMBL 靶标：AN3-CA External Id：CHEMBL5135788

实验名称：Anti-migratory activity against human J82 cells harboring FGFR3 K652E mutant incubate... 来源：ChEMBL 靶标：J82 External Id：CHEMBL5135789

实验名称：Anti-invasive activity against against human AN3-CA cells harboring FGFR2 K310R/N549K... 来源：ChEMBL 靶标：AN3-CA External Id：CHEMBL5135790

实验名称：Anti-invasive activity against against human J82 cells harboring FGFR3 K652E mutant a... 来源：ChEMBL 靶标：J82 External Id：CHEMBL5135791

实验名称：Induction of cell cycle arrest in human AN3-CA cells assessed as accumulation of cell... 来源：ChEMBL 靶标：AN3-CA External Id：CHEMBL5135784

实验名称：Induction of cell cycle arrest in human KMS-11 cells assessed as accumulation of cell... 来源：ChEMBL 靶标：KMS-11 External Id：CHEMBL5135785

实验名称：Induction of cell cycle arrest in human J82 cells assessed as accumulation of cells a... 来源：ChEMBL 靶标：J82 External Id：CHEMBL5135786

实验名称：Induction of cell cycle arrest in mouse BaF3 cells harboring TEL-V555M-FGFR3 mutant a... 来源：ChEMBL 靶标：BaF3 External Id：CHEMBL5135787

实验名称：Induction of apoptosis in mouse BaF3 cells harboring TEL-V555M-FGFR3 mutant assessed ... 来源：ChEMBL 靶标：BaF3 External Id：CHEMBL5135780

实验名称：Induction of apoptosis in human KMS-11 cells assessed as increase in cleaved caspase-... 来源：ChEMBL 靶标：KMS-11 External Id：CHEMBL5135781

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