Compound 15 PARP/PI3K inhibitor (RGNCY-0128)
Per 10 mg
Compound 15 is a novel potent dual PARP/PI3K inhibitor. Compound 15 effectively inhibits PARP-1/2 and PI3K-alpha/delta with antiprolferative effects against both BRCA-deficient and BRCA-proficient cancer cells in cellular assays. Compound 15 was shown to have a greater in vivo anti-tumor efficacy than the drug combination of Olaparib and BKM120 in the MDA-MB-468 xenograft mouse model with 74% inhibition without observable toxicity. These data suggest that compound 15 is a potent dual PARP/PI3K inhibitor and may be an effective anti-cancer treatment.
Systematic Name: N-(4-ethyl-3-(morpholinosulfonyl)phenyl)-3-(1H-pyrrol-1-yl)benzamide
Mol Wt: 439.53
Wang J et al. Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3‑Kinase Inhibitors as a Promising Strategy for Cancer Therapy. J. Med. Chem. (2020) 63, 122−139.
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