MK-4827 (tosylate)

MK-4827 is an orally bioavailable inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 3.8 and 2.1 nM, respectively). It inhibits the proliferation of cancer cells carrying the breast cancer mutations BRCA1 and BRCA2 in vitro (IC50 values range from 10-100 nM) and has efficacy alone against a xenograft of BRCA1-deficient cancer in mice. MK-4827 sensitizes human lung and breast cancer xenografts to radiation in mice. Formulations containing MK-4827 are effective against ovarian cancer, particularly in platinum-sensitive, recurrent ovarian cancer.Formal Name: 2-[4-(3S)-3-piperidinylphenyl]-2H-indazole-7-carboxamide, 4-methylbenzenesulfonate. CAS Number: 1038915-73-9. Synonyms: Niraparib tosylate. Molecular Formula: C19H20N4O . C7H8O3S. Formula Weight: 492.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml, Ethanol: 1 mg/ml. lambdamax: 223, 239, 311 nm. SMILES: NC(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C21)=O.CC5=CC=C(S(O)(=O)=O)C=C5. InChi Code: InChI=1S/C19H20N4O.C7H8O3S/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14,1-6-2-4-7(5-3-6)11(8,9)10/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24),2-5H,1H3,(H,8,9,10)/t14-,/m1./s1. InChi Key: LCPFHXWLJMNKNC-PFEQFJNWSA-N.