| Identification | Back Directory | [Name]
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 | [CAS]
2839740-79-1 | [Synonyms]
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
8H-Purin-8-imine, 2-(4-cyclopropyl-6-methoxy-5-pyrimidinyl)-7,9-dihydro-9-[[4-[1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl]phenyl]methyl]-7-(2,2,2-trifluoroethyl)- | [Molecular Formula]
C27H23F6N9O | [MOL File]
2839740-79-1.mol | [Molecular Weight]
603.52 |
| Chemical Properties | Back Directory | [Boiling point ]
641.3±65.0 °C(predicted) | [density ]
1.58±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
2.60±0.60(predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
TNG348 is an orally available allosteric inhibitor of the ubiquitin-specific protease USP1. TNG348 specifically and efficiently inhibits the activity of USP1, inhibiting its deubiquitination of proliferative PCNA and FANCD2, thereby disrupting the DNA repair process. TNG348 has inhibitory activity against breast and ovarian cancers carrying BRCA1/2 mutations and other homologous recombination defects (HRD) [1][2]. | [IC 50]
JNK1 | [References]
[1] Simoneau A, et al. Abstract B054: TNG348, a selective USP1 inhibitor, shows strong preclinical combination activity with PARP inhibitors and other agents targeting DNA repair[J]. Molecular Cancer Therapeutics, 2023, 22 (12_Supplement) : B054-B054.
[2] Previtali V, et al. New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives. J Med Chem. 2024 Jul 25;67 (14) :11488-11521. DOI:10.1021/acs.jmedchem.4c00113 |
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