Chemical Structure : TNG348
CAS No.: 2839740-79-1
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 | |
25 mg | Get quote | ||
100 mg | Get quote |
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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.
分子量 | 603.53 | |
分子式 | C27H23F6N9O | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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 |
1. Simoneau A, et al. Mol Cancer Ther. 2025 Jan 31. doi: 10.1158/1535-7163.MCT-24-0515.
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