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AZD 2281 - Olaparib - KU 0059436

 

 

CAS 763113-22-0 

C24H23FN4O3 MW 434.47

Purity: 99%

 

 

 

 

 

Ordering Information:

 

Cat. No. Axon 1464      Promotion      

 

1 x 5 mg / 75  $98

Promotion: 10 mg @ 100  $130

1 x 25 mg / 200  $260

Promotion: 50 mg @ 300  $390

Bulk on request

 

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*fully QCed drug standard, COA/MSDS available

 

Biological Activity:

 

Highly potent, oral and selective inhibitor of poly(ADP-ribose) polymerase (PARP); with IC50 = 5 nM (PARP1) and 1 nM (PARP2). It blocks enzymes that repair DNA damage caused by cancer treatments such as radiation and drugs.

 

References: online        List of Publications Using Axon 1464

 

S Vasiliou et al. Olaparib. Drugs of the Future. 2009, 34(2), 101.

 

KA Menear 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, 51(20), 65816591. [online]

 

S Rottenberg et al. High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs. Proc. Nat. Acad. Sci. USA, 2008, 105(44), 1707984. [online]

 

T Hay et al. Poly(ADP-ribose) polymerase-1 inhibitor treatment regresses autochthonous Brca2/p53-mutant mammary tumors in vivo and delays tumor relapse in combination with carboplatin. Cancer Res. 2009, 69(9), 3850. [online]

 

C Mitchell et al. Poly(ADP-Ribose) Polymerase 1 Modulates the Lethality of CHK1 Inhibitors in Carcinoma Cells. Mol. Pharmacol. 2010, 78(5), 909-917. [online]

 

 

Chemical Name: 4-[(3-{[4-Cyclopropylcarbonyl)piperazin-4-yl]carbonyl}-4-fluorophenyl)methyl]phtalazin-1(2H)-one

 

AZD 2281 - Olaparib | PARP inhibitor | Axon 1464 | AZD2281 from supplier Axon Medchem

 

Axon Ligands TM - Research chemicals for biological study. Some high-profile samples could be provided under terms of contract research synthesis.

axonmedchem.com 2014

 

Axon Ligands in the field:

 

3-AB | PARP inhibitor

ABT 888 | PARP inhibitor

AG 014699 | PARP inhibitor

AZD 2461 | PARP inhibitor

DR 2313 | PARP inhibitor

Iniparib | PARP inhibitor

KU 0058948 | PARP inhibitor

NU 1025 | PARP inhibitor

Olaparib | PARP inhibitor

 

 

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