AZD2281/KU 59436

Min.Order / FOB Price:Get Latest Price

100 Gram	FOB Price: USD 1.0000

100 Gram

FOB Price: USD 1.0000

Min.Order :100 Gram
Purity: 98%
Payment Terms : L/C

Keywords

KU 59436 Olaparib;1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine;Olaparib(AZD-2281);Azd 2281;Azd2281;Azd-2281;Ku-0059436;4-[3-(4-Cyclopropanecarbonyl-piperaz 763113-22-0

Quick Details

Appearance:white powder
Application:CAS：763113-22-0； Olaparib;1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine;Olaparib(AZD-2281);Azd 2281;Azd2281;Azd-2281;Ku-0059436;4-[3-(4-Cyclopro
PackAge:100g,500,1kg.....
ProductionCapacity:100|Metric Ton|Week
Storage:Dry seal
Transportation:shipping

Superiority:

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Details:

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 μM). 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.

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