Formulation: A solid
Formal Name: 4-[[3-[[5,6-dihydro-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone
Purity: ≥98%
Formula Markup: C22H16F4N6O2
CAS Number: 1358715-18-0
Notes: Fluzoparib is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; IC50 = 1.46 nM).{68675} It induces DNA double-strand breaks in wild-type, but not BRCA2-/-, V-C8 cells, as well as BRCA1-/- MDA-MB-436 cells when used at concentrations of 1 and 10 µM. Fluzoparib inhibits the proliferation of BRCA2-/- V-C8 cells (IC50 = 0.053 µM), BRCA1-/- MDA-MB-436, UWB1.289, and MX-1 cells (IC50s = 0.51, 1.57, and 1.57 µM, respectively), and OVCAR-8 cells containing hypermethylated BRCA1 (IC50 = 1.43 µM). In vivo, fluzoparib (1 and 3 mg/kg) reduces tumor formation in an MDA-MB-436 mouse xenograft model.
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