Bulk Inquiry
Olaparib
- AZD2281 - KU-0059436
- Soluble in DMSO
- MF: C24H23FN4O3
- MW: 434.46
Description
Olaparib (AZD2281) is a highly potent, orally active and selective poly(ADP-ribose) polymerase (PARP) inhibitor with IC50 values of 5 nM for PARP1 and 1 nM for PARP2. Olaparib inhibits PARP-mediated DNA repair pathways, resulting in the accumulation of DNA damage and enhanced sensitivity of cancer cells to DNA-damaging agents.
PARP1 and PARP2 are key enzymes involved in the repair of single-strand DNA breaks through the base excision repair pathway. Inhibition of PARP activity leads to persistent DNA damage, replication stress, and synthetic lethality in cells with defects in homologous recombination repair, including BRCA1- and BRCA2-mutant cancers. Olaparib is widely used in DNA damage response (DDR), oncology, and genome stability research.
Key Features
- Highly potent PARP1 and PARP2 inhibitor
- IC50: 5 nM for PARP1 and 1 nM for PARP2
- Orally active compound
- Suppresses PARP-mediated DNA repair
- Widely used tool for DNA damage response research
Applications
- PARP and DNA repair research
- DNA damage response (DDR) studies
- BRCA and homologous recombination deficiency research
- Cancer biology and synthetic lethality investigations
- Genome stability and replication stress studies
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
Related Products
| AXON ID | NAME | FROM PRICE |
|---|---|---|
| 1268 | DR 2313 |
From $99.00 |
| 1370 | NU 1025 |
From $88.00 |
| 1496 | 3-Aminobenzamide |
From $44.00 |
| 1529 | AG 014699 |
From $66.00 |
| 1566 | Iniparib |
From $66.00 |
| 1593 | Veliparib |
From $44.00 |
| 2001 | KU-0058948 hydrochloride |
From $148.50 |
| 2241 | AZD2461 |
From $104.50 |
| 2369 | UPF 1069 |
From $82.50 |
| 2502 | Talazoparib |
From $99.00 |
| 2759 | ME0328 |
From $104.50 |
| 2885 | GeA-69 |
From $104.50 |
| 2888 | Veliparib dihydrochloride |
From $99.00 |
| 2928 | Niraparib |
From $99.00 |
| 3113 | Rucaparib camsylate |
From $99.00 |
| 3398 | E7449 mesylate |
From $121.00 |
| 3795 | PDD00017273 |
From $99.00 |
| 4179 | KU-0058948 |
From $148.50 |
| 4276 | AG14361 |
From $143.00 |
| 4435 | RBN-2397 |
From $198.00 |
