TRK-IN-24

• 常用名: TRK-IN-24
• 英文名: TRK-IN-24
• CAS号: 2937544-01-7
• 分子量: 659.82
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₉H₄₅N₇O₃
• 熔点: N/A
• 闪点: N/A

TRK-IN-24用途

TRK-IN-24 (compound 10g) 是 Trk Receptor 抑制剂,抑制 TRKA、TRKC、TRKAG595R、TRKAG667C 和 TRKAF589L 的 IC50s 分别为 5.21、4.51、6.77、1.42 和 6.13 nM。TRK-IN-24 在 BaF3-CD74-NTRK1G595R 和 BaF3-CD74-NTRK1G667C 异种移植模型中具有抗肿瘤功效。TRK-IN-24 抑制转染 SF、GK、xDFG等单突变体的 Ba/F3 细胞的增殖,IC50 为 1.43-47.56 nM。

TRK-IN-24名称

• 英文名: TRK-IN-24

TRK-IN-24生物活性

• 描述: TRK-IN-24 (compound 10g) 是 Trk Receptor 抑制剂,抑制 TRKA、TRKC、TRKAG595R、TRKAG667C 和 TRKAF589L 的 IC50s 分别为 5.21、4.51、6.77、1.42 和 6.13 nM。TRK-IN-24 在 BaF3-CD74-NTRK1G595R 和 BaF3-CD74-NTRK1G667C 异种移植模型中具有抗肿瘤功效。TRK-IN-24 抑制转染 SF、GK、xDFG等单突变体的 Ba/F3 细胞的增殖,IC50 为 1.43-47.56 nM。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 蛋白酪氨酸激酶 >> Trk Receptor
• 靶点实验:

  IC50: 5.21 nM (TRKA), 4.51 nM (TRKC), 6.77 nM (TRKAG595R), 1.42 nM (TRKAG667C), 6.13 nM (TRKAF589L)[1]

• 参考文献:

  [1]. Wang Z, et al. Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations. J Med Chem. 2023 Sep 7.. .

TRK-IN-24物理化学性质

• 分子式: C₃₉H₄₅N₇O₃
• 分子量: 659.82
• InChIKey: YOBIWCLAYQWPPW-UHFFFAOYSA-N
• SMILES: Cc1c2cc(cc1C(=O)Nc1cc(CN3CCN(C)CC3)cc(C3CC3)c1)OCCCCCCCNC(=O)c1ccc3ncc(n3n1)C#C2

TRK-IN-24靶点实验

查看更多实验

实验名称：Inhibition of Musk (unknown origin) at 1000 nM relative to control 来源：ChEMBL 靶标：Muscle, skeletal receptor tyrosine-protein kinase External Id：CHEMBL5367773

实验名称：Inhibition of RET (unknown origin) at 1000 nM relative to control 来源：ChEMBL 靶标：Proto-oncogene tyrosine-protein kinase receptor Ret External Id：CHEMBL5367771

实验名称：Inhibition of FLT4 (unknown origin) at 1000 nM relative to control 来源：ChEMBL 靶标：Vascular endothelial growth factor receptor 3 External Id：CHEMBL5367772

实验名称：Inhibition of Mer (unknown origin) at 1000 nM relative to control 来源：ChEMBL 靶标：Tyrosine-protein kinase Mer External Id：CHEMBL5367769

实验名称：Inhibition of P70S6K (unknown origin) at 1000 nM relative to control 来源：ChEMBL 靶标：Ribosomal protein S6 kinase beta-2 External Id：CHEMBL5367770

实验名称：Inhibition of Hck (unknown origin) at 1000 nM relative to control 来源：ChEMBL 靶标：Tyrosine-protein kinase HCK External Id：CHEMBL5367767

实验名称：Inhibition of KDR (unknown origin) at 1000 nM relative to control 来源：ChEMBL 靶标：Vascular endothelial growth factor receptor 2 External Id：CHEMBL5367768

实验名称：Inhibition of wild type TRKA G667C mutant in mouse BaF3 cells measured after 6 hrs by... 来源：ChEMBL 靶标：High affinity nerve growth factor receptor External Id：CHEMBL5367829

实验名称：Inhibition of Tie2 (unknown origin) at 1000 nM relative to control 来源：ChEMBL 靶标：Angiopoietin-1 receptor External Id：CHEMBL5367765

实验名称：Inhibition of wild type TRKA V573M mutant in mouse BaF3 cells measured after 6 hrs by... 来源：ChEMBL 靶标：High affinity nerve growth factor receptor External Id：CHEMBL5367830

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