MK-4827 tosylate

White to off-white solid. Soluble in DMSO or DMF (both 20mg/ml). Sparingly soluble in ethanol (1mg/ml) or water (<1mg/ml). Chemical. CAS: 1038915-73-9. Formula: C19H20N4O . C7H8O3S. MW: 492.6. Synthetic. MK-4827 is an orally bioavailable inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s=3.8 and 2.1nM, respectively). It inhibits the proliferation of cancer cells carrying the breast cancer mutations BRCA1 and BRCA2 in vitro 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.3 Formulations containing MK-4827 are effective against ovarian cancer.