For research use only. Not for therapeutic Use.
Rubitecan is a semisynthetic agent related to camptothecin with potent antitumor and antiviral properties. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks.
| Catalog Number | R007201 |
| CAS Number | 91421-42-0 |
| Synonyms | (4S)-4-Ethyl-4-hydroxy-10-nitro-1H-pyrano[3’,4’:6,7]indolizinol[1,2-b]quinoline-3,?14(4H,-12H)-dione; 9-Nitrocamptothecin; 9-NC; Orathecin; |
| Molecular Formula | C20H15N3O6 |
| Purity | ≥95% |
| Target | Topoisomerase |
| Storage | -20°C |
| InChI | InChI=1S/C20H15N3O6/c1-2-20(26)13-7-16-17-10(8-22(16)18(24)12(13)9-29-19(20)25)6-11-14(21-17)4-3-5-15(11)23(27)28/h3-7,26H,2,8-9H2,1H3/t20-/m0/s1 |
| InChIKey | VHXNKPBCCMUMSW-FQEVSTJZSA-N |
| SMILES | CCC1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=CC=C(C5=C4)[N+](=O)[O-])O |
| Reference | </br>1:Phase II study of rubitecan in recurrent or metastatic head and neck cancer. Caponigro F, Cartenì G, Droz JP, Milano A, Davis WB, Pollard P.Cancer Chemother Pharmacol. 2008 Jul;62(2):209-14. Epub 2007 Sep 19. PMID: 17882418 </br>2:Phase II study of rubitecan, an oral camptothecin in patients with advanced colorectal cancer who have failed previous 5-fluorouracil based chemotherapy. Patel H, Stoller R, Auber M, Potter D, Cai C, Zamboni W, Kiefer G, Matin K, Schmotzer A, Ramanathan RK.Invest New Drugs. 2006 Jul;24(4):359-63. PMID: 16525767 </br>3:Rubitecan. Clark JW.Expert Opin Investig Drugs. 2006 Jan;15(1):71-9. Review. PMID: 16370935 </br>4:Minimal clinical benefit of single agent Orathecin (Rubitecan) in heavily pretreated metastatic breast cancer. Chedid S, Rivera E, Frye DK, Ibrahim N, Esteva F, Valero V, Hortobagyi G, Mettinger KL, Cristofanilli M.Cancer Chemother Pharmacol. 2006 Apr;57(4):540-4. Epub 2005 Sep 29. PMID: 16193332 </br>5:A phase II trial with RFS2000 (rubitecan) in patients with advanced non-small cell lung cancer. Baka S, Ranson M, Lorigan P, Danson S, Linton K, Hoogendam I, Mettinger K, Thatcher N.Eur J Cancer. 2005 Jul;41(11):1547-50. PMID: 16026691 </br>6:Phase II trial of oral rubitecan in previously treated pancreatic cancer patients. Burris HA 3rd, Rivkin S, Reynolds R, Harris J, Wax A, Gerstein H, Mettinger KL, Staddon A.Oncologist. 2005 Mar;10(3):183-90. PMID: 15793221 Free Article</br>7:Rubitecan: 9-NC, 9-Nitro-20(S)-camptothecin, 9-nitro-camptothecin, 9-nitrocamptothecin, RFS 2000, RFS2000. [No authors listed]Drugs R D. 2004;5(5):305-11. PMID: 15357630 </br>8:Development of an optimal pharmacokinetic sampling schedule for rubitecan administered orally in a daily times five schedule. Schoemaker NE, Mathôt RA, Schöffski P, Rosing H, Schellens JH, Beijnen JH.Cancer Chemother Pharmacol. 2002 Dec;50(6):514-7. Epub 2002 Nov 5. PMID: 12451480 </br>9:Phase I study of rubitecan and gemcitabine in patients with advanced malignancies. Fracasso PM, Rader JS, Govindan R, Herzog TJ, Arquette MA, Denes A, Mutch DG, Picus J, Tan BR, Fears CL, Goodner SA, Sun SL.Ann Oncol. 2002 Nov;13(11):1819-25. PMID: 12419757 </br>10:Preclinical activity of an i.v. formulation of rubitecan in IDD-P against human solid tumor xenografts. Sands H, Mishra A, Stoeckler JD, Hollister B, Chen SF.Anticancer Drugs. 2002 Oct;13(9):965-75. PMID: 12394260 |
