Olaparib-d5

Olaparib-d5 (AZD2281-d5) is the deuterium labeled Olaparib (HY-10162) . Olaparib 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

[2143107-56-4]

Product Name Alternative

AZD2281-d5; KU0059436-d5

UNSPSC

12352005

Target

Autophagy; Isotope-Labeled Compounds; Mitophagy; PARP

Type

Isotope-Labeled Compounds

Related Pathways

Autophagy; Cell Cycle/DNA Damage; Epigenetics; Others

Applications

Cancer-programmed cell death

Field of Research

Cancer

Purity

99.37

Solubility

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

Smiles

O=C1NN=C(CC2=CC=C(F)C(C(N3CCN(C(C4([2H])C([2H])([2H])C4([2H])[2H])=O)CC3)=O)=C2)C5=C1C=CC=C5

Molecular Formula

C24H18D5FN4O3

Molecular Weight

439.49

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.