Rucaparib, 25 mg

Offered by STEMCELL Technologies, this cell-permeable small molecule acts as a poly ADP ribose polymerase (PARP) inhibitor, with a reported PARP1 Ki < 5 nM. It also inhibits PARP2, 3, 4, 12, 15, and 16, as well as tankyrase 1 and 2, and shows selectivity for PARP in human cancer cells carrying BRCA-1 or BRCA-2 mutations. DNA breaks normally activate PARP, which promotes repair of DNA damage through relaxation of chromatin and recruitment of other repair proteins; by inhibiting this activity, the compound leads to DNA damage and cancer cell death.

Alternative names include AG014699 and PF01367338. The CAS number is 283173-50-2, the chemical formula is C19H18FN3O, and the molecular weight is 323.4 g/mol. Reported purity is ≥ 98%. The chemical name is 8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one. The material is supplied as a yellow powder.

The product is stable at -20°C as supplied; STEMCELL recommends storing small molecules away from direct light, with a desiccant for long-term storage. It is stable as supplied for 12 months from date of receipt. Solubility in DMSO is ≤ 75 mM, and the compound has low solubility in aqueous media. For cell culture use, stock solution should be diluted into culture medium immediately before use, with final DMSO concentration kept below 0.1% due to potential cell toxicity. Published cancer research applications include antagonism of multidrug resistance in doxorubicin- and paclitaxel-resistant cervical cancer cell lines, cytotoxicity in human cell lines with mutated BRCA1/2, reduction of mouse xenograft tumor growth with BRCA1/2 mutations or epigenetically silenced BRCA1, and concentration-dependent antiproliferative effects in ovarian cancer cell lines. For research use only.