tcsc0075 Olaparib

Olaparib (AZD2281;KU0059436) is a potent and oral PARP inhibitor with IC₅₀s of 5 and 1 nM for PARP1 and PARP2, respectively.

IC50 & Target: IC50: 5/1 nM (PARP-1/2)^[1]

In Vitro: Olaparib (AZD2281) is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Olaparib is applied to SW620 cell lysates, and identified the IC₅₀ for PARP-1 inhibition to be around 6 nM and the total ablation of PARP-1 activity to be at concentrations of 30−100 nM^[1].

In Vivo: Animals bearing SW620 xenografted tumors are treated with Olaparib (10 mg/kg, p.o.) in combination with Temozolomide (TMZ) (50 mg/kg, p.o.) once daily for 5 consecutive days, after which the tumors are left to grow out^[1]. Olaparib increases vascular perfusion in Calu-6 tumors established in a DWC model. Administration of olaparib(50 mg/kg, p.o.) as a single agent (top panel) or in combination with radiation (bottom panel) results in an increase in fluorescence intensity in the Calu-6 tumors^[2].