Olaparib [763113-22-0]

Catalog number: HY-10162_100mg
Brand: MedChem Express
Packing: 100 mg
Other sizes: Also available in other sizes.
Price: € 139.00
Expected delivery time: 10 days
Olaparib Chemical Structure
CAS No. : 763113-22-0...

Product specifications for - Olaparib [763113-22-0]

Product group: Chemicals
Category: Other
CAS No.: 763113-22-0
Purity: >98%
Molecular Formula: C24H23FN4O3
Molecular weight: 434.46
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: Olaparib (AZD2281, KU0059436) is a potent PARP inhibitor with IC50 of 5 and 1 nM for PARP-1and PARP-2, respectively. IC50 Value: 5 nM(PARP-1), 1 nM(PARP-2) Target: PARP in vitro: Olaparib would act against BRCA1 or BRCA2 mutations. Olaparib is not sensitive to tankyrase-1 (IC50 >1 uM). Olaparib could ablate the PARP-1 activity at concentrations of 30-100 nM in SW620 cells. Olaparib is hypersensitive to BRCA1-deficient cell lines (MDA-MB-463 and HCC1937), compared with BRCA1- and BRCA2-proficient cell lines (Hs578T, MDA-MB-231, and T47D). Olaparib is strongly sensitive to KB2P cells due to suppression of base excision repair by PARP inhibition, which may result in the conversion of single-strand breaks to double-strand breaks during DNA replication, thus activating BRCA2-dependent recombination pathways. in vivo: Olaparib shows great response to Brca1-/-,p53-/- mammary tumors (50 mg/kg i.p. per day), while no responses to HR-deficient Ecad-/-,p53-/- mammary tumors. Olaparib even does not show dose-limiting toxicity in tumor-bearing mice. Olaparib has been used to treat with BRCA mutated tumors, such as ovarian, breast and prostate cancers. Moreover, Olaparib shows selectively inhibition to ATM (Ataxia Telangiectasia Mutated)-deficient tumor cells, which indicates to be a potential agent for treating ATM mutant lymphoid tumors.
Safety information: 
Additional information: 
Synonyms: HY-10162; AZD2281; KU0059436
Drug Driven Synthetic Lethality: bypassing tumor cell genetics with a combination of Dbait and PARPinhibitors.', Jdey W. Clin Cancer Res. 2017 Feb 15;23(4):1001-1011. Read more
Synthetic lethality in malignant pleural mesothelioma with PARP1 inhibition', Srinivasan G. Cancer Chemother Pharmacol. 2017 Oct;80(4):861-867. Read more
Hinokitiol copper complex inhibits proteasomal deubiquitination and induces paraptosis-like cell death in human cancer cells', Chen X. Eur J Pharmacol. 2017 Nov 15;815:147-155. Read more