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AZD2461
- Soluble in DMSO
- MF: C22H22FN3O3
- MW: 395.43
Description
AZD2461 is a potent, orally available PARP inhibitor with IC50 values of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively. It reduced P-glycoprotein substrate liability compared with earlier PARP inhibitors. It can retain activity in P-gp-proficient tumor models and in settings linked to 53BP1-dependent PARP inhibitor resistance.
PARP enzymes support single-strand DNA break repair and are important targets in synthetic-lethal oncology research. AZD2461 is valuable for studying DNA repair dependency, PARP inhibitor resistance mechanisms and the impact of drug efflux on antitumor efficacy.
Key Features
- Potent, orally available PARP inhibitor
- IC50 values: 5 nM for PARP1 and 2 nM for PARP2
- Reduced P-glycoprotein substrate profile
- Useful for studying PARP inhibitor resistance
Applications
- DNA damage response research
- PARP inhibitor pharmacology
- Drug-resistance and P-gp efflux studies
- Synthetic lethality and oncology models
More Information
| Parent CAS No. | 1174043-16-3 |
|---|---|
| Chemical Name | 4-(4-fluoro-3-(4-methoxypiperidine-1-carbonyl)benzyl)phthalazin-1(2H)-one |
| SMILES | C1C=C2C(=O)NN=C(CC3C=CC(F)=C(C(N4CCC(OC)CC4)=O)C=3)C2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C22H22FN3O3/c1-29-15-8-10-26(11-9-15)22(28)18-12-14(6-7-19(18)23)13-20-16-4-2-3-5-17(16)21(27)25-24-20/h2-7,12,15H,8-11,13H2,1H3,(H,25,27) |
| InChiKey | HYNBNUYQTQIHJK-UHFFFAOYSA-N |
| CID | 44199317 |
| Short Description | PARP inhibitor |
References
- J.E. Jaspers et al. Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov. 2013, 3, 68-81.
- K.A. Menear et al. Phthalazinone derivatives and their pharmaceutical compositions as PARP inhibitors useful for the treatment of diseases and preparation thereof. PCT Int. Appl. 2009, WO2009093032A1.
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