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TNG348

Chemical Structure : TNG348

CAS No.: 2839740-79-1

TNG348 (TNG-348)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 603.53
Formula C27H23F6N9O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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