Olaparib | CAS:763113-22-0

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Name:Olaparib; AZD2281; KU0059436
Cat. No. :CS-0075
CAS No. :763113-22-0
Formula:C24H23FN4O3
M. Wt. :434.46
Solubility:DMSO: 100 mg/mL, DMF: 50 mg/mL, Ethanol: 3.12 mg/mL

Olaparib is a potent PARP inhibitor with IC50 of 5 and 1 nM for PARP-1 and PARP-2, 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].

Senra JM, et al. Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft.Mol Cancer Ther. 2011 Oct;10(10):1949-58. Menear KA, et al. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91 Bian X, et al. PTEN deficiency sensitizes endometrioid endometrial cancer to compound PARP-PI3K inhibition but not PARP inhibition as monotherapy. Oncogene. 2018 Jan 18;37(3):341-351. Yasukawa M, et al. Synergetic Effects of PARP Inhibitor AZD2281 and Cisplatin in Oral Squamous Cell Carcinoma in Vitro and in Vivo. Int J Mol Sci. 2016 Feb 24;17(3):272.