763113-22-0

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AZD2281(olaparib)/AZD-2281/KU0059436

763113-22-0

Cat.No.ABP000423 Chemical NameAZD2281(olaparib)/AZD-2281/KU0059436 MolFormulaC24H23FN4O3 MolWeight434.4628 Purity 99%

Chemical Name : AZD2281(olaparib)/AZD-2281/KU0059436

CAS : 763113-22-0

Synonyms: 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine

Solubility:Soluble in DMSO, weakly in EtOH

Storage:-20C 2 years

Biologieal

AZD2281(olaparib) is a highly potent and selective phtalazinone-type PARP-inhibitor with IC 50 of 5nM (PARP-1) and 1 nM (PARP-2). AZD2281(olaparib)shows activity in BRCA-1 deficient breast cancer cells. Cell-kill in the presence of the alkylator methylmethansulfonate is potentiated by a factor of 25

Reference

1, 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.
Menear KA, J Med Chem. 2008 Oct 23;51(20):6581-91.


2, Poly(ADP-Ribose) Polymerase-1 Inhibitor Treatment Regresses Autochthonous Brca2/p53-Mutant Mammary Tumors In vivo and Delays Tumor Relapse in Combination with Carboplatin.
Hay T, Cancer Res. 2009 Apr 21.

3, High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs.
Rottenberg S, Proc Natl Acad Sci U S A. 2008 Nov 4;105(44):17079-84.

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