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PP-048

Chemical Structure : PP-048

CAS No.:

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PP-048 (PP048)

Catalog No.: PC-28106Not For Human Use, Lab Use Only.

PP-048 is a potent, selective, second-generation dual inhibitor of Polθ and PARP1 with IC50 of 4.9 nM and 6.8 nM, respectively, shows >226-fold selectivity over PARP2, PARP3, PARP5a/b, and PARP7.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PP-048 is a potent, selective, second-generation dual inhibitor of Polθ and PARP1 with IC50 of 4.9 nM and 6.8 nM, respectively, shows >226-fold selectivity over PARP2, PARP3, PARP5a/b, and PARP7.
PP-048 (10 mg/kg) achieved marked tumor growth inhibition (TGI = 91%) without eliciting the hematologic toxicity in MDA-MB-436 xenograft model.

Physicochemical Properties

M.Wt 733.25
Formula C37H33ClN10O3S
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'-chloro-N-(5-((5-(4-((7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)pyridin-2-yl)ethynyl)-1,3,4-thiadiazol-2-yl)-5'-methoxy-6-methyl-[4,4'-bipyridine]-3-carboxamide

References

1. Ma L, et al. J Med Chem. 2026 Sep 10;69(17):20651-20677.

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