IDH2R140Q-IN-2

• 常用名: IDH2R140Q-IN-2
• 英文名: IDH2R140Q-IN-2
• CAS号: 2749568-16-7
• 分子量: 484.40
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₁H₁₈F₆N₆O
• 熔点: N/A
• 闪点: N/A

IDH2R140Q-IN-2用途

IDH2R140Q-IN-2 (化合物 36) 是一种具有口服活性的 IDH2R140Q 抑制剂 (IC50: 29 nM)。IDH2R140Q-IN-2 减少表达突变 IDH2R140Q 的 TF-1 细胞系中 D2HG 的产生 (IC50: 10 nM)。IDH2R140Q-IN-2 抑制肿瘤组织中的 D2HG 水平。IDH2R140Q-IN-2 可用于急性髓系白血病 (AML) 的研究。

IDH2R140Q-IN-2名称

• 英文名: IDH2R140Q-IN-2

IDH2R140Q-IN-2生物活性

• 描述: IDH2R140Q-IN-2 (化合物 36) 是一种具有口服活性的 IDH2R140Q 抑制剂 (IC50: 29 nM)。IDH2R140Q-IN-2 减少表达突变 IDH2R140Q 的 TF-1 细胞系中 D2HG 的产生 (IC50: 10 nM)。IDH2R140Q-IN-2 抑制肿瘤组织中的 D2HG 水平。IDH2R140Q-IN-2 可用于急性髓系白血病 (AML) 的研究。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 代谢酶/蛋白酶 >> 异柠檬酸脱氢酶(IDH)
• 参考文献:

  [1]. Wei Q, et al. Structure-Based Drug Design of Novel Triaminotriazine Derivatives as Orally Bioavailable IDH2R140Q Inhibitors with High Selectivity and Reduced hERG Inhibitory Activity for the Treatment of Acute Myeloid Leukemia. J Med Chem. 2023 Sep 28;66(18):12894-12910.

IDH2R140Q-IN-2物理化学性质

• 分子式: C₂₁H₁₈F₆N₆O
• 分子量: 484.40

IDH2R140Q-IN-2靶点实验

查看更多实验

实验名称：Toxicity in NCG mouse xenografted with human TF-1 cells expressing IDH2 R140Q mutant ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5368547

实验名称：Antitumor activity against human TF-1 cells expressing IDH2 R140Q mutant xenografted ... 来源：ChEMBL 靶标：TF-1 External Id：CHEMBL5368548

实验名称：Toxicity in NCG mouse xenografted with human TF-1 cells expressing IDH2 R140Q mutant ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5368545

实验名称：Toxicity in NCG mouse xenografted with human TF-1 cells expressing IDH2 R140Q mutant ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5368546

实验名称：Induction of hematopoietic differentiation in EPO-induced human TF-1 cells expressing... 来源：ChEMBL 靶标：TF-1 External Id：CHEMBL5368543

实验名称：Toxicity in NCG mouse xenografted with human TF-1 cells expressing IDH2 R140Q mutant ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5368544

实验名称：MRT in BALB/c mouse at 25 mg/kg, po measured upto 72 hrs by LC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL5368541

实验名称：Oral bioavailability in BALB/c mouse at 25 mg/kg measured upto 72 hrs by LC-MS/MS ana... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5368542

实验名称：AUC (0 to infinity) in BALB/c mouse at 25 mg/kg, po measured upto 72 hrs by LC-MS/MS ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5368540

实验名称：Clearance in BALB/c mouse at 5 mg/kg, iv measured for 24 hrs by LC-MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL5368537

共29条，当前第1页，共3页

1

2

3