For research use only. Not for therapeutic Use.
Tasisulam CAT No.: R023705 , also known as LY573636, is an acyl-sulfonamide with potential antineoplastic activity. Selectively toxic towards tumor cells, tasisulam appears to induce tumor cell apoptosis by a mitochondrial-targeted mechanism involving the loss of mitochondrial membrane potential and induction of reactive oxygen species (ROS). In combination with an angiogenesis inhibitor, this agent may exhibit synergistic antiangiogenic activity.
| Catalog Number | R023705 |
| CAS Number | 519055-62-0 |
| Synonyms | N-[(5-Bromo-2-thienyl)sulfonyl]-2,4-dichloro-benzamide; LY 573636; N-(2,4-Dichlorobenzoyl)-5-bromothiophene-2-sulfonamide |
| Molecular Formula | C11H6BrCl2NO3S2 |
| Purity | ≥95% |
| Target | Apoptosis |
| Storage | -20°C |
| IUPAC Name | N-(5-bromothiophen-2-yl)sulfonyl-2,4-dichlorobenzamide |
| InChI | InChI=1S/C11H6BrCl2NO3S2/c12-9-3-4-10(19-9)20(17,18)15-11(16)7-2-1-6(13)5-8(7)14/h1-5H,(H,15,16) |
| InChIKey | WWONFUQGBVOKOF-UHFFFAOYSA-N |
| SMILES | C1=CC(=C(C=C1Cl)Cl)C(=O)NS(=O)(=O)C2=CC=C(S2)Br |
| Reference | </br>1:Synthesis of a Sulfonimidamide-Based Analog of Tasisulam and Its Biological Evaluation in the Melanoma Cell Lines SKMel23 and A375. Steinkamp AD, Schmitt L, Chen X, Fietkau K, Heise R, Baron JM, Bolm C.Skin Pharmacol Physiol. 2016;29(6):281-290. doi: 10.1159/000453042. Epub 2016 Dec 24. PMID: 28013301 </br>2:An innovative, multi-arm, complete phase 1b study of the novel anti-cancer agent tasisulam in patients with advanced solid tumors. Jotte RM, Von Hoff DD, Braiteh F, Becerra CR, Richards DA, Smith DA, Garbo L, Stephenson J, Conkling PR, Robert-Vizcarrondo F, Chen J, Turner PK, Chow KH, Tai DF, Ilaria R Jr.Invest New Drugs. 2015 Feb;33(1):148-58. doi: 10.1007/s10637-014-0160-z. Epub 2014 Sep 28. PMID: 25260842 </br>3:A randomized, open-label clinical trial of tasisulam sodium versus paclitaxel as second-line treatment in patients with metastatic melanoma. Hamid O, Ilaria R Jr, Garbe C, Wolter P, Maio M, Hutson TE, Arance A, Lorigan P, Lee J, Hauschild A, Mohr P, Hahka-Kemppinen M, Kaiser C, Turner PK, Conti I, Grob JJ.Cancer. 2014 Jul 1;120(13):2016-24. doi: 10.1002/cncr.28635. Epub 2014 Mar 26. PMID: 24676877 Free Article</br>4:A phase I study of tasisulam sodium using an albumin-tailored dose in Japanese patients with advanced solid tumors. Fujiwara Y, Ando Y, Mukohara T, Kiyota N, Chayahara N, Mitsuma A, Inada-Inoue M, Sawaki M, Ilaria R Jr, Kellie Turner P, Funai J, Maeda K, Minami H.Cancer Chemother Pharmacol. 2013 Apr;71(4):991-8. doi: 10.1007/s00280-013-2092-2. Epub 2013 Feb 1. PMID: 23370664 </br>5:A phase I study of tasisulam sodium (LY573636 sodium), a novel anticancer compound, administered as a 24-h continuous infusion in patients with advanced solid tumors. Gordon MS, Ilaria R Jr, de Alwis DP, Mendelson DS, McKane S, Wagner MM, Look KY, LoRusso PM.Cancer Chemother Pharmacol. 2013 Jan;71(1):21-7. doi: 10.1007/s00280-012-1917-8. Epub 2012 Dec 11. PMID: 23228983 </br>6:Tasisulam sodium (LY573636 sodium) as third-line treatment in patients with unresectable, metastatic non-small-cell lung cancer: a phase-II study. Scagliotti GV, Ilaria R Jr, Novello S, von Pawel J, Fischer JR, Ermisch S, de Alwis DP, Andrews J, Reck M, Crino L, Eschbach C, Manegold C.J Thorac Oncol. 2012 Jun;7(6):1053-7. doi: 10.1097/JTO.0b013e3182519d79. PMID: 22588156 Free Article</br>7:A phase II study of tasisulam sodium (LY573636 sodium) as second-line or third-line treatment for patients with unresectable or metastatic soft tissue sarcoma. Ryan CW, Matias C, Agulnik M, Lopez-Pousa A, Williams C, de Alwis DP, Kaiser C, Miller MA, Ermisch S, Ilaria R Jr, Keohan ML.Invest New Drugs. 2013 Feb;31(1):145-51. doi: 10.1007/s10637-012-9819-5. Epub 2012 Apr 27. PMID: 22539091 </br>8:Tasisulam sodium, an antitumor agent that inhibits mitotic progression and induces vascular normalization. Meier T, Uhlik M, Chintharlapalli S, Dowless M, Van Horn R, Stewart J, Blosser W, Cook J, Young D, Ye X, Evans G, Credille K, Ballard D, Huber L, Capen A, Chedid M, Ilaria R Jr, Smith MC, Stancato L.Mol Cancer Ther. 2011 Nov;10(11):2168-78. doi: 10.1158/1535-7163.MCT-11-0323. Epub 2011 Sep 8. PMID: 21903607 Free Article</br>9:A phase 2 study of tasisulam sodium (LY573636 sodium) as second-line treatment for patients with unresectable or metastatic melanoma. Kirkwood JM, Gonzalez R, Reintgen D, Clingan PR, McWilliams RR, de Alwis DP, Zimmermann A, Brown MP, Ilaria RL Jr, Millward MJ.Cancer. 2011 Oct 15;117(20):4732-9. doi: 10.1002/cncr.26068. Epub 2011 Mar 31. PMID: 21456002 Free Article</br>10:A phase I study of tasisulam sodium (LY573636 sodium), a novel anticancer compound in patients with refractory solid tumors. Simon GR, Ilaria RL Jr, Sovak MA, Williams CC, Haura EB, Cleverly AL, Sykes AK, Wagner MM, de Alwis DP, Slapak CA, Miller MA, Spriggs DR.Cancer Chemother Pharmacol. 2011 Nov;68(5):1233-41. doi: 10.1007/s00280-011-1593-0. Epub 2011 Mar 23. PMID: 21431416 Free PMC Article |
