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Olaparib-d4-1

Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib. 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

2143107-55-3

Product Name Alternative

AZD2281-d4-1; KU0059436-d4-1

UNSPSC

12352005

Target

Autophagy; Isotope-Labeled Compounds; Mitophagy; PARP

Type

Isotope-Labeled Compounds

Related Pathways

Autophagy; Cell Cycle/DNA Damage; Epigenetics; Others

Field of Research

Cancer

Purity

98.59

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=C(N1CCN(CC1)C(C2=C(C=CC(CC(C3=C4C=CC=C3)=NNC4=O)=C2)F)=O)C5C([2H])(C5([2H])[2H])[2H]

Molecular Formula

C24H19D4FN4O3

Molecular Weight

438.49

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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.|[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]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|[5]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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Isotope-Labeled Compounds

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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