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AG 014699
- PF 01367338 - Rucaparib
- Parent CAS: 283173-50-2
- Soluble in water and DMSO
- MF: C19H18FN3O.H3O4P
- MW: 421.36
Description
AG 014699 (Rucaparib) is a highly potent and orally active PARP inhibitor that blocks poly(ADP-ribose) polymerase activity involved in single-strand DNA break repair.
PARP inhibition is central to DNA damage response research and synthetic-lethality strategies in homologous recombination-deficient tumor models. AG 014699 is relevant for studying chemosensitization, radiosensitization and PARP-dependent repair mechanisms.
Key Features
- Highly potent PARP inhibitor, primarily targeting PARP1 (Ki: 1.4 nM), PARP2 and PARP3
- Blocks PARP-mediated DNA repair signaling
- Relevant to synthetic-lethality studies in DNA repair-deficient models
- Useful chemosensitizing and radiosensitizing research tool
Applications
- DNA damage response research
- PARP inhibitor pharmacology
- BRCA and homologous recombination-deficient cancer models
- Chemotherapy and radiation combination studies
Note: AG-014699 is the phosphate salt of AG 014447 (CAS 283173-50-2) and has improved aqueous solubility. Another salt form, Rucaparib camsylate (Axon 3113) is also available.
More Information
| Parent CAS No. | 283173-50-2 |
|---|---|
| Chemical Name | 8-Fluoro-2-(4-methylaminomethyl-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one phosphate |
| SMILES | C1(C2NC3C=C(F)C=C4C(=O)NCCC=2C=34)C=CC(CNC)=CC=1.P(=O)(O)(O)O |
| MFCD | MFCD11977252 |
| InChi | InChI=1S/C19H18FN3O.H3O4P/c1-21-10-11-2-4-12(5-3-11)18-14-6-7-22-19(24)15-8-13(20)9-16(23-18)17(14)15;1-5(2,3)4/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24);(H3,1,2,3,4) |
| InChiKey | FCCGJTKEKXUBFZ-UHFFFAOYSA-N |
| CID | 9931953 |
| Short Description | PARP1 inhibitor |
References
- HD Thomas et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol. Cancer Ther. 2007, 6(3), 945-56.
- P Plummer et al. Phase I study of the poly(ADP-ribose) polymerase inhibitor, AG014699, in combination with temozolomide in patients with advanced solid tumors. Clin Cancer Res. 2008, 14(23), 7917-23.
- M Ali et al. Vasoactivity of AG014699, a Clinically Active Small Molecule Inhibitor of Poly(ADP-ribose) Polymerase: a Contributory Factor to Chemopotentiation In vivo? Clin. Cancer Res. 2009, 15(19), 6106-6112.
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