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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Deubiquitinase (DUB)-TNG348
TNG348

Chemical Structure : TNG348

CAS No.: 2839740-79-1

TNG348 (TNG-348)

货号: PC-24036Not For Human Use, Lab Use Only.

TNG348 is a potent, a selective, allosteric and reversible USP1 inhibitor with IC50 of 98.6 nM in AlphaLISA-based measurement of ub-PCNA induction in MDA-MB-436 cells.

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2 mg ¥1980 In stock
5 mg ¥3280 In stock
10 mg ¥5280 In stock
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100 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TNG348 is a potent, a selective, allosteric and reversible USP1 inhibitor with IC50 of 98.6 nM in AlphaLISA-based measurement of ub-PCNA induction in MDA-MB-436 cells.
TNG348 induces a dose-dependent loss of viability in the BRCA1-mutant MDA-MB-436 cell line with an average IC50 of 68.3 nM, while having no impact on the BRCA1 WT HCC1954 cell line.
TNG348 exhibits high selectivity in a panel of 47 DUBs (Ubiquigent), including USP12 and USP46, as well as against 467 of the 468 kinases tested.
TNG348 is active in BRCA mutant and HRD+ breast and ovarian cancer cells and acts through a distinct mechanism from PARPi.
TNG348 synergizes with PARPi and other DNA-damaging agents in HRD+ and BRCA-mutant cell lines.
TNG348 drives strong antitumor activity in combination with PARPi in HRD+ models and can overcome PARPi resistance.

物理化学性质&存储条件

分子量 603.53
分子式 C27H23F6N9O
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)-9-(4-(1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl)benzyl)-7-(2,2,2-trifluoroethyl)-7,9-dihydro-8H-purin-8-imine

参考文献

1. Simoneau A, et al. Mol Cancer Ther. 2025 Jan 31. doi: 10.1158/1535-7163.MCT-24-0515.

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