Fluzoparib

Fluzoparib is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1, IC50 = 1.46 nM). 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.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. CAS Number: 1358715-18-0. Molecular Formula: C22H16F4N6O2. Formula Weight: 472.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble. SMILES: O=C1NN=C(CC2=CC=C(C(C(N3CC4=NC(C(F)(F)F)=NN4CC3)=O)=C2)F)C5=C1C=CC=C5. InChi Code: InChI=1S/C22H16F4N6O2/c23-16-6-5-12(10-17-13-3-1-2-4-14(13)19(33)29-28-17)9-15(16)20(34)31-7-8-32-18(11-31)27-21(30-32)22(24,25)26/h1-6,9H,7-8,10-11H2,(H,29,33). InChi Key: XJGXCBHXFWBOTN-UHFFFAOYSA-N.