Olaparib, 100 mg

STEMCELL Technologies supplies a small molecule identified as a potent, cell-permeable inhibitor of poly ADP ribose polymerase (PARP), with affinity for both PARP1 and PARP2 (IC50 = 5 and 1 nM; Menear et al.). The compound acts as an inhibitor of PARPs in cancer cells harbouring BRCA1 or BRCA2 mutations. Mechanistically, DNA breaks normally activate PARPs, which promote 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 (Davar et al.).

Alternative names are AZD-2281 and KU-59436. The chemical formula is C24H23FN4O3, with a molecular weight of 434.5 g/mol and a purity of ≥ 98%. It is supplied as an off-white powder and is stable at -20°C as supplied for 12 months from date of receipt. STEMCELL recommends storing all small molecules away from direct light, and for long-term storage, storing with a desiccant. Reported solubility is ≤ 75 mM in DMSO and ≤ 3.9 mM in absolute ethanol. To prepare a 10 mM stock solution in DMSO, 10 mg should be resuspended in 2.30 mL of DMSO, and stock solutions should be prepared fresh before use. The compound has low solubility in aqueous media, and for use as a cell culture supplement, stock solution should be diluted into culture medium immediately before use, avoiding final DMSO or absolute ethanol concentration above 0.1% due to potential cell toxicity.

Published cancer research applications include inhibition of tumor growth and overall survival in ATM-deficient mantle cell lymphoma cells, inhibition of growth of esophageal squamous cell carcinoma cells by cell cycle arrest at G2/M, induction of anti-proliferative effects in specific endometrial cancer cell lines, reported efficacy against epithelial ovarian cancer, prevention or partial reversion of EMT induced by TGF-β in NMuMG cells, and prevention of OVA-induced airway inflammation and remodelling in mice through modulation of inflammasome signalling. The product is for research use only and is not intended for human or animal diagnostic or therapeutic uses.