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1.
Rucaparib, CAS#: 283173-50-2 (free base), HPLC 99.2%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 100g in stock.
Name: Rucaparib free base
CAS#: 283173-50-2 (free base)
Chemical Formula: C19H18FN3O
Exact Mass: 323.1434
Molecular Weight: 323.3714
Elemental Analysis: C, 70.57; H, 5.61; F, 5.88; N, 12.99; O, 4.95
Related CAS #: 283173-50-2 (free base) 459868-92-9 (phosphate) 1859053-21-6 (Rucaparib camsylate)
Synonym: Rucaparib free base, AG-14447; AG 14447; AG14447; Rubraca.
IUPAC/Chemical Name: 8-Fluoro-2-(4-((methylamino)methyl)phenyl)-1,3,4,5-tetrahydro-6H-azepino(5,4,3-cd)indol-6-one
InChi Key: HMABYWSNWIZPAG-UHFFFAOYSA-N
InChiCode:InChI=1S/C19H18FN3O/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/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24)
SMILES Code: O=C1NCCC2=C(C3=CC=C(CNC)C=C3)NC4=C2C1=CC(F)=C4
Appearance: Yellow solid powder
2.
Rucaparib intermediates:
Rucaparib intermediate, Rucaparib Camsylate, CAS#1859053-21-6, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Rucaparib intermediate,5-Fluoro-2-Methyl-3-nitrobenzoic acid, CAS#850462-64-5, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Rucaparib intermediate,5-Fluoro-2-methylbenzoic acid, CAS#33184-16-6, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Rucaparib intermediate,5-FLUORO-2-METHYL-3-NITRO-BENZOIC ACID METHYL ESTER, CAS#697739-03-0, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Rucaparib intermediate, 6-Fluoro-1H-indole-4-carboxylic acid methyl ester, CAS#1082040-43-4 , HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Rucaparib intermediate, 8-fluoro-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one, CAS#1408282-26-7, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Rucaparib intermediate, 2-bromo-8-fluoro-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one, CAS#283173-80-8, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
Rucaparib intermediate, 4-(8-fluoro-6-oxo-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-2-yl)benzaldehyde, CAS#283173-84-2, HPLC 99%, HNMR, C13-NMR, MASS, MSDS, COA, MOA all we provided, More than 10kg in stock.
REFERENCES
1: Parrish KE, Cen L, Murray J, Calligaris D, Kizilbash S, Mittapalli RK, Carlson BL, Schroeder MA, Sludden J, Boddy AV, Agar NY, Curtin NJ, Elmquist WF, Sarkaria JN. Efficacy of PARP Inhibitor Rucaparib in Orthotopic Glioblastoma Xenografts Is Limited by Ineffective Drug Penetration into the Central Nervous System. Mol Cancer Ther. 2015 Dec;14(12):2735-43. doi: 10.1158/1535-7163.MCT-15-0553. PubMed PMID: 26438157; PubMed Central PMCID: PMC4674360.
2: McCrudden CM, O'Rourke MG, Cherry KE, Yuen HF, O'Rourke D, Babur M, Telfer BA, Thomas HD, Keane P, Nambirajan T, Hagan C, O'Sullivan JM, Shaw C, Williams KJ, Curtin NJ, Hirst DG, Robson T. Vasoactivity of rucaparib, a PARP-1 inhibitor, is a complex process that involves myosin light chain kinase, P2 receptors, and PARP itself. PLoS One. 2015 Feb 17;10(2):e0118187. doi: 10.1371/journal.pone.0118187. PubMed PMID: 25689628; PubMed Central PMCID: PMC4331495.
3: Murray J, Thomas H, Berry P, Kyle S, Patterson M, Jones C, Los G, Hostomsky Z, Plummer ER, Boddy AV, Curtin NJ. Tumour cell retention of rucaparib, sustained PARP inhibition and efficacy of weekly as well as daily schedules. Br J Cancer. 2014 Apr 15;110(8):1977-84. doi: 10.1038/bjc.2014.91. PubMed PMID: 24556618; PubMed Central PMCID: PMC3992512.
4: Durmus S, Sparidans RW, van Esch A, Wagenaar E, Beijnen JH, Schinkel AH. Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1) restrict oral availability and brain accumulation of the PARP inhibitor rucaparib (AG-014699). Pharm Res. 2015 Jan;32(1):37-46. doi: 10.1007/s11095-014-1442-z. PubMed PMID: 24962512.
5: Falzacappa MV, Ronchini C, Faretta M, Iacobucci I, Di Rorà AG, Martinelli G, Meyer LH, Debatin KM, Orecchioni S, Bertolini F, Pelicci PG. The Combination of the PARP Inhibitor Rucaparib and 5FU Is an Effective Strategy for Treating Acute Leukemias. Mol Cancer Ther. 2015 Apr;14(4):889-98. doi: 10.1158/1535-7163.MCT-14-0276. PubMed PMID: 25667168.
6: Ihnen M, zu Eulenburg C, Kolarova T, Qi JW, Manivong K, Chalukya M, Dering J, Anderson L, Ginther C, Meuter A, Winterhoff B, Jones S, Velculescu VE, Venkatesan N, Rong HM, Dandekar S, Udar N, Jänicke F, Los G, Slamon DJ, Konecny GE. Therapeutic potential of the poly(ADP-ribose) polymerase inhibitor rucaparib for the treatment of sporadic human ovarian cancer. Mol Cancer Ther. 2013 Jun;12(6):1002-15. doi: 10.1158/1535-7163.MCT-12-0813. PubMed PMID: 23729402; PubMed Central PMCID: PMC3963026.
7: Wilson RH, Evans TJ, Middleton MR, Molife LR, Spicer J, Dieras V, Roxburgh P, Giordano H, Jaw-Tsai S, Goble S, Plummer R. A phase I study of intravenous and oral rucaparib in combination with chemotherapy in patients with advanced solid tumours. Br J Cancer. 2017 Feb 21. doi: 10.1038/bjc.2017.36. [Epub ahead of print] PubMed PMID: 28222073.
8: Swisher EM, Lin KK, Oza AM, Scott CL, Giordano H, Sun J, Konecny GE, Coleman RL, Tinker AV, O'Malley DM, Kristeleit RS, Ma L, Bell-McGuinn KM, Brenton JD, Cragun JM, Oaknin A, Ray-Coquard I, Harrell MI, Mann E, Kaufmann SH, Floquet A, Leary A, Harding TC, Goble S, Maloney L, Isaacson J, Allen AR, Rolfe L, Yelensky R, Raponi M, McNeish IA. Rucaparib in relapsed, platinum-sensitive high-grade ovarian carcinoma (ARIEL2 Part 1): an international, multicentre, open-label, phase 2 trial. Lancet Oncol. 2017 Jan;18(1):75-87. doi: 10.1016/S1470-2045(16)30559-9. PubMed PMID: 27908594.
9: Drew Y, Ledermann J, Hall G, Rea D, Glasspool R, Highley M, Jayson G, Sludden J, Murray J, Jamieson D, Halford S, Acton G, Backholer Z, Mangano R, Boddy A, Curtin N, Plummer R. Phase 2 multicentre trial investigating intermittent and continuous dosing schedules of the poly(ADP-ribose) polymerase inhibitor rucaparib in germline BRCA mutation carriers with advanced ovarian and breast cancer. Br J Cancer. 2016 Mar 29;114(7):723-30. doi: 10.1038/bjc.2016.41. PubMed PMID: 27002934; PubMed Central PMCID: PMC4882768.
10: Wang DD, Li C, Sun W, Zhang S, Shalinsky DR, Kern KA, Curtin NJ, Sam WJ, Kirkpatrick TR, Plummer R. PARP activity in peripheral blood lymphocytes as a predictive biomarker for PARP inhibition in tumor tissues - A population pharmacokinetic/pharmacodynamic analysis of rucaparib. Clin Pharmacol Drug Dev. 2015 Mar;4(2):89-98. doi: 10.1002/cpdd.176. PubMed PMID: 27128213.
11: Murai J, Huang SY, Renaud A, Zhang Y, Ji J, Takeda S, Morris J, Teicher B, Doroshow JH, Pommier Y. Stereospecific PARP trapping by BMN 673 and comparison with olaparib and rucaparib. Mol Cancer Ther. 2014 Feb;13(2):433-43. doi: 10.1158/1535-7163.MCT-13-0803. PubMed PMID: 24356813; PubMed Central PMCID: PMC3946062.
12: Rucaparib Approved for Ovarian Cancer. Cancer Discov. 2017 Feb;7(2):120-121. doi: 10.1158/2159-8290.CD-NB2016-164. PubMed PMID: 28057616.
13: Sparidans RW, Durmus S, Schinkel AH, Schellens JH, Beijnen JH. Liquid chromatography-tandem mass spectrometric assay for the PARP inhibitor rucaparib in plasma. J Pharm Biomed Anal. 2014 Jan;88:626-9. doi: 10.1016/j.jpba.2013.10.016. PubMed PMID: 24216281.
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