Olaparib (AZD-2281, KU-0059436, KU 59436, Lynparza, 763113-22-0)

LC Laboratories' Product Number O-9201 - Olaparib (AZD-2281, KU-0059436, KU 59436, Lynparza, 763113-22-0), >99% - for research use only. Olaparib is a poly(ADP-ribose) polymerase 1 (PARP1) inhibitor and an anti-cancer drug being tested in patients with mutations in the genes BRCA1 or BRCA2. PARP1 acts as a critical molecule in the repair of DNA single-strand breaks (SSBs) and plays an important role in maintaining DNA integrity. PARP inhibitors inhibit PARP1 during S-phase and induce inactivation of SSB repair and thus cause DNA double-strand breaks, which induces BRCA-deficient cancer cell apoptosis. The PARP inhibitor olaparib was tested in a genetically engineered mouse model for BRCA1-associated breast cancer. Olaparib inhibited tumor growth and significantly improved survival without signs of toxicity. Long-term treatment with olaparib caused the development of drug resistance, which was induced by up-regulation of Abcb1a/b genes encoding P-glycoprotein efflux pumps. The resistance to olaparib could be overcome by tariquidar, a P-glycoprotein inhibitor. Combination treatment using olaparib with cisplatin or carboplatin improved the recurrence-free and overall survival in a murine model, indicating that olaparib enhances the effect of these DNA-damaging agents. Olaparib inhibited the growth of BRCA2-deficient versus BRCA2-proficient mammary tumor cells. Combination treatment of olaparib and cisplatin had a synergistic cytotoxicity against BRCA2-deficient cells but not against BRCA2-proficient control cells. Other CAS numbers previously assigned to olaparib, namely 894104-70-2, 937799-91-2, and 1021843-02-6, have been deleted by CAS and are no longer in use.

• Supplier: LC Laboratories
• Product #: O-9201
• Sku #: O-9201_1g