Olaparib

• 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].

• Product Name Alternative:

  AZD2281; KU0059436

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  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:

  DMSO : 100 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 Formula:

  C24H23FN4O3

• Molecular Weight:

  434.46

• Precautions:

  H302, H315, H319, H335

• 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)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  PARP1; PARP2; TNKS1/PARP5A

• CAS Number:

  [763113-22-0]