Olaparib

• UNSPSC Description:

  Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].

• Target Antigen:

  Autophagy; Mitophagy; PARP

• Type:

  Reference compound

• Related Pathways:

  Autophagy;Cell Cycle/DNA Damage;Epigenetics

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Olaparib.html

• Purity:

  99.98

• Solubility:

  DMF : 50 mg/mL (ultrasonic)|DMSO : 100 mg/mL (ultrasonic)|Ethanol : 3.12 mg/mL (ultrasonic;warming;heat to 60°C)

• Smiles:

  O=C(C1=CC(CC(C2=C3C=CC=C2)=NNC3=O)=CC=C1F)N4CCN(C(C5CC5)=O)CC4

• Molecular Weight:

  434.46

• References & Citations:

  [1]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|[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.|[3]Yasukawa M, et al. Synergetic Effects of PARP Inhibitor AZD2281 in Oral Squamous Cell Carcinoma in Vitro and in Vivo. Int J Mol Sci. 2016 Feb 24;17(3):272.|[4]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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Launched

• CAS Number:

  763113-22-0