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Olaparib
- AZD2281 - KU-0059436
- Soluble in DMSO
- MF: C24H23FN4O3
- MW: 434.46
Description
Highly potent, oral and selective inhibitor of poly(ADP-ribose) polymerase (PARP); with IC50 = 5nM (PARP-1) and 1 nM (PARP-2). It blocks enzymes that repair DNA damage caused by cancer treatments such as radiation and drugs.
More Information
| Parent CAS No. | 763113-22-0 |
|---|---|
| Chemical Name | 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one |
| SMILES | C1=CC2C(=O)NN=C(CC3C=C(C(=O)N4CCN(C(C5CC5)=O)CC4)C(F)=CC=3)C=2C=C1 |
| MFCD | MFCD13185161 |
| InChi | InChI=1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30) |
| InChiKey | FDLYAMZZIXQODN-UHFFFAOYSA-N |
| CID | 23725625 |
| Short Description | PARP inhibitor |
References
- 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), 6581–6591.
- 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), 17079–84.
- 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.
- 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.
- List of publications using Olaparib (Axon 1464) purchased from Axon Medchem
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