Chemical Structure : TNG-6132
CAS No.:
2821749-57-7
TNG-6132
(TNG6132)
Catalog No.: 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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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505.51
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Formula
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C26H22F3N7O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(4-cyclopropyl-6-methoxypyrimidin-5-yl)-7-(4-(1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl)benzyl)-5H-pyrrolo[3,2-d]pyrimidine
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References
1. Throner S, et al. Bioorg Med Chem Lett. 2025 Apr 30:130262.
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