Rucaparib Camsylate

• CAS: 1859053-21-6
• Catalog Number: ACM1859053216
• Category: Inhibitors
• Molecular Weight: 555.67
• Molecular Formula: C29H34FN3O5S
• Description: Rucaparib camsylate is a potent, orally available inhibitor of poly ADP-ribose polymerase (PARP) 1 and 2.
• Synonyms: AG14699 (as phosphate salt); AG 14699; AG-14699; AG014447 (as free base); AG-014447; AG 014447; PF01367338; PF-01367338; PF 01367338; Rucaparib camsylate; Rubraca
• IUPAC Name: Bicyclo(2.2.1)heptane-1-methanesulfonic acid, 7,7-dimethyl-2-oxo-, (1S,4R)-, compd. with 8-fluoro-1,3,4,5-tetrahydro-2-(4-((methylamino)methyl)phenyl)-6H-pyrrolo(4,3,2-ef)(2)benzazepin-6-one (1:1)
• Canonical SMILES: O=S(C[C@@]1(C2(C)C)C(C[C@@]2([H])CC1)=O)(O)=O.O=C(NCC3)C4=CC(F)=CC5=C4C3=C(C6=CC=C(CNC)C=C6)N5
• InChI: INBJJAFXHQQSRW-STOWLHSFSA-N
• InChI Key: InChI=1S/C19H18FN3O.C10H16O4S/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;1-9(2)7-3-4-10(9,8(11)5-7)6-15(12,13)14/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24);7H,3-6H2,1-2H3,(H,12,13,14)/t;7-,10-/m.1/s1
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >3 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Alternative CAS: 283173-50-2 (free base); 459868-92-9 (phosphate);1859053-21-6 (camsylate)
• Biological Target: Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains.
• Drug Formulation: This drug may be formulated in DMSO
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: The ability of p65 to bind with its consensus sequence following either IR or TNF-α in p65+/+ or p65-/- MEFs was investigated. SiRNA targeting p65 or a combination of p65 siRNA and AG-014699 reduced DNA binding > 85% following IR in p65+/+ cells (p=0.008 and p=0.009, compared to IR alone, respectively). PARP-1 siRNA inhibited DNA binding by approximately 60% (p= 0.03, compared to IR). Significantly, AG-014699 also reduced IR-induced DNA binding to levels comparable with untreated controls (p=0.05, compared to IR). p65 siRNA or a combination of p65 siRNA and AG-014699 reduced DNA binding to levels relative to Mock treated controls, following TNF-α (p= 0.009 and p=0.007, compared to TNF-α alone, respectively). Importantly, PARP-1 siRNA also reduced DNA binding 25% after TNF-α treatment (p=0.02, compared to TNF-α).; Reference: Oncogene. 2012 Jan 12;31(2):251-64. https://pubmed.ncbi.nlm.nih.gov/21706052/
• In Vivo Activity: Vessel mismatch was markedly reduced in the AG14361 (10 mg/kg) pre-treated SW620 xenografts compared to control (18 versus 51%). Vessel mismatch was also reduced following AG014699 (1 mg/kg; 28%) and nicotinamide (1 g/kg; 19%) pre-treatment. Thus, AG014699 has a similar effect to a 10x higher concentration of AG14361 and a 1,000x higher concentration of nicotinamide. For AG014699 the amount of vessel closure was further reduced compared with AG14361 and nicotinamide to only 5% in mice treated with AG014699. Furthermore the proportion of vessels open at the time of carbocyanine injection was greater in AG014699 treated mice (21%) compared with AG14361 and nicotinamide (7% for both) and was comparable to controls. Furthermore the proportion of vessels open at the time of carbocyanine injection was greater in AG014699 treated mice (21%) compared with AG14361 and nicotinamide (7% for both), indicating that a substantial amount of the vessel mismatch was a consequence of vessel opening.; Reference: Clin Cancer Res. 2009 Oct 1;15(19):6106-12. https://pubmed.ncbi.nlm.nih.gov/19789326/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).