Rucaparib phosphate
CAS#: 459868-92-9 (phosphate)
Description: Rucaparib, also known as (AG-14699 or PF-01367338, is a tricyclic indole poly(ADP-Ribose) polymerase (PARP1) inhibitor with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Rucaparib selectively binds to PARP1 and inhibits PARP1-mediated DNA repair, thereby enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy.
Synonym: AG14699 (as phosphate salt); AG 14699; AG-14699; AG014447 (as free base); AG-014447; AG 014447; PF01367338; PF-01367338; PF 01367338; Rucaparib.
IUPAC/Chemical Name: 8-fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one phosphate
THEORETICAL ANALYSIS
Name: Rucaparib phosphate
CAS#: 459868-92-9 (phosphate)
Chemical Formula: C19H18FN3O
Exact Mass: 323.14339
Molecular Weight: 323.36
Elemental Analysis:
TECHNICAL DATA
ADDITIONAL INFORMATION
Related CAS#
CAS#459868-92-9 ( Rucaparib phosphate salt)
CAS#283173-50-2 (Rucaparib free base)
REFERENCES
1: Sun Y, Ding H, Liu X, Li X, Li L. INPP4B overexpression enhances the antitumor efficacy of PARP inhibitor AG014699 in MDA-MB-231 triple-negative breast cancer cells. Tumour Biol. 2014 Jan 14. [Epub ahead of print] PubMed PMID: 24420152.
2: Plummer R, Lorigan P, Steven N, Scott L, Middleton MR, Wilson RH, Mulligan E, Curtin N, Wang D, Dewji R, Abbattista A, Gallo J, Calvert H. A phase II study of the potent PARP inhibitor, Rucaparib (PF-01367338, AG014699), with temozolomide in patients with metastatic melanoma demonstrating evidence of chemopotentiation. Cancer Chemother Pharmacol. 2013 May;71(5):1191-9. doi: 10.1007/s00280-013-2113-1. Epub 2013 Feb 20. PubMed PMID: 23423489.
3: Ali M, Kamjoo M, Thomas HD, Kyle S, Pavlovska I, Babur M, Telfer BA, Curtin NJ, Williams KJ. The clinically active PARP inhibitor AG014699 ameliorates cardiotoxicity but does not enhance the efficacy of doxorubicin, despite improving tumor perfusion and radiation response in mice. Mol Cancer Ther. 2011 Dec;10(12):2320-9. doi: 10.1158/1535-7163.MCT-11-0356. Epub 2011 Sep 16. PubMed PMID: 21926192; PubMed Central PMCID: PMC3242069.
4: Drew Y, Mulligan EA, Vong WT, Thomas HD, Kahn S, Kyle S, Mukhopadhyay A, Los G, Hostomsky Z, Plummer ER, Edmondson RJ, Curtin NJ. Therapeutic potential of poly(ADP-ribose) polymerase inhibitor AG014699 in human cancers with mutated or methylated BRCA1 or BRCA2. J Natl Cancer Inst. 2011 Feb 16;103(4):334-46. doi: 10.1093/jnci/djq509. Epub 2010 Dec 23. PubMed PMID: 21183737.
5: Ali M, Telfer BA, McCrudden C, O’Rourke M, Thomas HD, Kamjoo M, Kyle S, Robson T, Shaw C, Hirst DG, Curtin NJ, Williams KJ. 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 Oct 1;15(19):6106-12. doi: 10.1158/1078-0432.CCR-09-0398. Epub 2009 Sep 29. PubMed PMID: 19789326; PubMed Central PMCID: PMC2756456.
6: Plummer R, Jones C, Middleton M, Wilson R, Evans J, Olsen A, Curtin N, Boddy A, McHugh P, Newell D, Harris A, Johnson P, Steinfeldt H, Dewji R, Wang D, Robson L, Calvert H. 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 Dec 1;14(23):7917-23. doi: 10.1158/1078-0432.CCR-08-1223. PubMed PMID: 19047122; PubMed Central PMCID: PMC2652879.
