Rucaparib (AG-014699)

Description: Rucaparib (formerly known as AG-014699 or PF-01367338; trade name: Rubraca) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, it also shows binding affinity to eight other PARP domains. In December 2016, Rucaparib was approved by FDA to treat women with a certain type of ovarian cancer. Rucaparib selectively binds to PARP1 and inhibits PARP1-mediated DNA repair, thereby enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy.

References: Mol Cancer Ther. 2007 Mar; 6(3):945-56; Br J Cancer. 2010 Nov 9; 103(10):1588-96.

Related CAS#:459868-92-9 (phosphate); 1859053-21-6 (Rucaparib camsylate)