For research use only. Not for therapeutic Use.
Rucaparib（Cat No.:I002961）is a potent oral poly (ADP-ribose) polymerase (PARP) inhibitor used in the treatment of advanced ovarian, fallopian tube, and primary peritoneal cancers with BRCA1/2 mutations. By inhibiting PARP enzymes, Rucaparib prevents cancer cells from repairing DNA damage, leading to cell death, particularly in tumors with deficient homologous recombination repair mechanisms, such as BRCA-mutated cancers. It is used both as a maintenance therapy and for treating recurrent cancers. Rucaparib’s targeted action makes it an important therapeutic option for improving progression-free survival in patients with specific genetic profiles.
| Catalog Number | I002961 |
| CAS Number | 283173-50-2 |
| Synonyms | 8-fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one |
| Molecular Formula | C19H18FN3O |
| Purity | 98% |
| Target | PARP |
| Target Protein | |
| Solubility | DMSO > 80 mg/ml; Water <1 mg/ml |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IC50 | PARP-1:1.4 nM (Ki) |
| IUPAC Name | 6-fluoro-2-[4-(methylaminomethyl)phenyl]-3,10-diazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13)-tetraen-9-one |
| InChI | 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) |
| InChIKey | HMABYWSNWIZPAG-UHFFFAOYSA-N |
| SMILES | CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)N2 |
| Reference | </br>1:Drug Monographs: Olaratumab and Rucaparib. Solimando DA Jr, Waddell JA.Hosp Pharm. 2017 Apr;52(4):258-263. doi: 10.1310/hpj5203-258. PMID: 28515503 </br>2:Activity of trabectedin and the PARP inhibitor rucaparib in soft-tissue sarcomas. Laroche A, Chaire V, Le Loarer F, Algéo MP, Rey C, Tran K, Lucchesi C, Italiano A.J Hematol Oncol. 2017 Apr 11;10(1):84. doi: 10.1186/s13045-017-0451-x. PMID: 28399901 Free PMC Article</br>3:A Phase I-II Study of the Oral PARP Inhibitor Rucaparib in Patients with Germline <i>BRCA1/2</i>-Mutated Ovarian Carcinoma or Other Solid Tumors. Kristeleit R, Shapiro GI, Burris HA, Oza AM, LoRusso P, Patel MR, Domchek SM, Balmaña J, Drew Y, Chen LM, Safra T, Montes A, Giordano H, Maloney L, Goble S, Isaacson J, Xiao J, Borrow J, Rolfe L, Shapira-Frommer R.Clin Cancer Res. 2017 Mar 6. doi: 10.1158/1078-0432.CCR-16-2796. [Epub ahead of print] PMID: 28264872 </br>4:Rucaparib: First Global Approval. Syed YY.Drugs. 2017 Apr;77(5):585-592. doi: 10.1007/s40265-017-0716-2. Review. PMID: 28247266 </br>5:A phase I study of intravenous and oral rucaparib in combination with chemotherapy in patients with advanced solid tumours. Wilson RH, Evans TJ, Middleton MR, Molife LR, Spicer J, Dieras V, Roxburgh P, Giordano H, Jaw-Tsai S, Goble S, Plummer R.Br J Cancer. 2017 Mar 28;116(7):884-892. doi: 10.1038/bjc.2017.36. Epub 2017 Feb 21. PMID: 28222073 Free PMC Article</br>6:Rucaparib Approved for Ovarian Cancer. [No authors listed]Cancer Discov. 2017 Feb;7(2):120-121. doi: 10.1158/2159-8290.CD-NB2016-164. Epub 2017 Jan 5. PMID: 28057616 </br>7:Genomic LOH May Predict Rucaparib Response in Ovarian Cancer. [No authors listed]Cancer Discov. 2017 Jan;7(1):OF8. doi: 10.1158/2159-8290.CD-RW2016-230. Epub 2016 Dec 9. PMID: 27940438 </br>8:Rucaparib in relapsed, platinum-sensitive high-grade ovarian carcinoma (ARIEL2 Part 1): an international, multicentre, open-label, phase 2 trial. 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.Lancet Oncol. 2017 Jan;18(1):75-87. doi: 10.1016/S1470-2045(16)30559-9. Epub 2016 Nov 29. PMID: 27908594 Free Article</br>9:Ovarian Cancers Harbor Defects in Nonhomologous End Joining Resulting in Resistance to Rucaparib. McCormick A, Donoghue P, Dixon M, O/’Sullivan R, O/’Donnell RL, Murray J, Kaufmann A, Curtin NJ, Edmondson RJ.Clin Cancer Res. 2017 Apr 15;23(8):2050-2060. doi: 10.1158/1078-0432.CCR-16-0564. Epub 2016 Oct 4. PMID: 27702817 </br>10:An evaluation in vitro of PARP-1 inhibitors, rucaparib and olaparib, as radiosensitisers for the treatment of neuroblastoma. Nile DL, Rae C, Hyndman IJ, Gaze MN, Mairs RJ.BMC Cancer. 2016 Aug 11;16:621. doi: 10.1186/s12885-016-2656-8. PMID: 27515310 Free PMC Article |
