Olaparib

A potent, specific, and orally active PARP inhibitor with IC50 of 5 and 1 nM for PARP1 and PARP2, respectively; displays 300-fold selectivity over tankyrase (TNKS-1 IC50=1.5 uM) ; shows standalone activity against BRCA1-deficient breast cancer cell lines; regresses autochthonous Brca2/p53-mutant mammary tumors in vivo and delays tumor relapse in combination with carboplatin.Ovarian Cancer Approved (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. (In Vivo) :Animals bearing SW620 xenografted tumors are treated with Olaparib (10 mg/kg, p.o.) in combination with NSC 362856 (TMZ) (50 mg/kg, p.o.) once daily for 5 consecutive days, after which the tumors are left to grow out. 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.

763113-22-0

AZD2281 | KU-0059436 | KU0059436 | | AZD 2281

Pharmacology & Drug Discovery

>98% (HPLC)

DMSO: 29 mg/mL

O=C1NN=C (CC2=CC=C (F) C (C (N3CCN (C (C4CC4) =O) CC3) =O) =C2) C5=C1C=CC=C5

C24H23FN4O3

434.4628

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.