Olaparib

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 Specifications

CAS Number

[763113-22-0]

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.