763113-22-0

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.