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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-TNG-6132
TNG-6132

Chemical Structure : TNG-6132

CAS No.: 2821749-57-7

TNG-6132 (TNG6132)

货号: PC-24549Not For Human Use, Lab Use Only.

TNG-6132 is a potent, selective, reversible, allosteric and orally bioavailable USP1 inhibitor with pIC50 of 7.9 (USP1-UAF1 complex), and pIC50 of 7.6 in cellular viability assay with MDA-MB-436 cells.

规格 价格 库存 数量
25 mg Get quote
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100 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

TNG-6132 is a potent, selective, reversible, allosteric and orally bioavailable USP1 inhibitor with pIC50 of 7.9 (USP1-UAF1 complex), and pIC50 of 7.6 in cellular viability assay with MDA-MB-436 cells.
TNG-6132 interacts non-covalently with the complex by binding to a cryptic allosteric pocket in USP1.
TNG-6132 (10, 30 and 100 mg/kg) resulted in a dose-proportional plasma exposure and dose-dependent increase in the pharmacodynamic marker ub-PCNA as measured in harvested tumor samples from MDA-MB-436 cell-derived murine xenograft model.
TNG-6132 (100 mg/kg, 200 mg/kg) reduced tumor volume in PARP inhibitor-resistant BRCA1-mutated patient-derived xenograft (PDX) murine model of ovarian cancer.

物理化学性质&存储条件

分子量 505.51
分子式 C26H22F3N7O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-7-(4-(1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl)benzyl)-5H-pyrrolo[3,2-d]pyrimidine

参考文献

1. Throner S, et al. Bioorg Med Chem Lett. 2025 Apr 30:130262.

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