PP-048

PP-048: sourced facts only. name: "This effort culminated in the discovery of compound PP-048 (23), a second-generation dual inhibitor with single-digit nanomolar potency against Polθ and PARP1 (IC50 = 4.9 nM and 6.8 nM, respectively) and >226-fold selectivity over PARP2, PARP3, PARP5a/b, and PARP7." [PMID:42720455]; target: "This effort culminated in the discovery of compound PP-048 (23), a second-generation dual inhibitor with single-digit nanomolar potency against Polθ and PARP1 (IC50 = 4.9 nM and 6.8 nM, respectively) and >226-fold selectivity over PARP2, PARP3, PARP5a/b, and PARP7." [PMID:42720455]; developer: "State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, College of Pharmacy, China Pharmaceutical University, Nanjing211198, P. R. China." [PMID:42720455]; stage: "In an MDA-MB-436 xenograft model, PP-048 (10 mg/kg) achieved marked tumor growth inhibition (TGI = 91%) without eliciting the hematologic toxicity associated with PARP2 inhibition." [PMID:42720455]