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AZD2461
- Soluble in DMSO
- MF: C22H22FN3O3
- MW: 395.43
Description
PARP inhibitor (IC50 value 5 nM) with poor P-glycoprotein substrate qualities. Unlike treatment with Olaparib (AZD2281; Axon 1464), AZD2461 succesfully circumvents drug resistance of Pgp-proficient tumors, and inactivation of p53-binding protein 1 (53BP1) as a causal factor in PARPi resistance.
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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