Tasisulam
Tasisulam, 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.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | Tasisulam |
|---|---|
| Iupac 化学名称 | N-(2,4-Dichlorobenzoyl)-5-bromothiophene-2-sulfonamide |
| 同义词 | LY573636, LY 573636, LY-573636, Tasisulam, Tasisulam sodium |
| 英文同义词 | LY573636, LY 573636, LY-573636, Tasisulam, Tasisulam sodium |
| 分子式 | C11H6BrCl2NO3S2 |
| 分子量 | 415.097 |
| Smile | O=S(C1=CC=C(Br)S1)(NC(C2=CC=C(Cl)C=C2Cl)=O)=O |
| InChiKey | WWONFUQGBVOKOF-UHFFFAOYSA-N |
| 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) |
| Cas号 | 519055-62-0 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: 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. An innovative, multi-arm, complete phase 1b study of the novel anti-cancer agent tasisulam in patients with advanced solid tumors. Invest New Drugs. 2014 Sep 28. [Epub ahead of print] PubMed PMID: 25260842.
2: 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. A randomized, open-label clinical trial of tasisulam sodium versus paclitaxel as second-line treatment in patients with metastatic melanoma. Cancer. 2014 Jul 1;120(13):2016-24. doi: 10.1002/cncr.28635. Epub 2014 Mar 26. PubMed PMID: 24676877.
3: 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. A phase I study of tasisulam sodium using an albumin-tailored dose in Japanese patients with advanced solid tumors. Cancer Chemother Pharmacol. 2013 Apr;71(4):991-8. doi: 10.1007/s00280-013-2092-2. Epub 2013 Feb 1. PubMed PMID: 23370664.
4: Gordon MS, Ilaria R Jr, de Alwis DP, Mendelson DS, McKane S, Wagner MM, Look KY, LoRusso PM. 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. Cancer Chemother Pharmacol. 2013 Jan;71(1):21-7. doi: 10.1007/s00280-012-1917-8. Epub 2012 Dec 11. PubMed PMID: 23228983.
5: Schindler K, Schicher N, Kunstfeld R, Pehamberger H, Toepker M, Haitel A, Hoeller C, Harmankaya K. A rare case of primary rhabdoid melanoma of the urinary bladder treated with ipilimumab, an anti-CTLA 4 monoclonal antibody. Melanoma Res. 2012 Aug;22(4):320-5. doi: 10.1097/CMR.0b013e32835566c0. PubMed PMID: 22713795.
6: 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. Tasisulam sodium (LY573636 sodium) as third-line treatment in patients with unresectable, metastatic non-small-cell lung cancer: a phase-II study. J Thorac Oncol. 2012 Jun;7(6):1053-7. doi: 10.1097/JTO.0b013e3182519d79. PubMed PMID: 22588156.
7: 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. 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. Invest New Drugs. 2013 Feb;31(1):145-51. doi: 10.1007/s10637-012-9819-5. Epub 2012 Apr 27. PubMed PMID: 22539091.
8: 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. Tasisulam sodium, an antitumor agent that inhibits mitotic progression and induces vascular normalization. Mol Cancer Ther. 2011 Nov;10(11):2168-78. doi: 10.1158/1535-7163.MCT-11-0323. Epub 2011 Sep 8. PubMed PMID: 21903607.
9: Kirkwood JM, Gonzalez R, Reintgen D, Clingan PR, McWilliams RR, de Alwis DP, Zimmermann A, Brown MP, Ilaria RL Jr, Millward MJ. A phase 2 study of tasisulam sodium (LY573636 sodium) as second-line treatment for patients with unresectable or metastatic melanoma. Cancer. 2011 Oct 15;117(20):4732-9. doi: 10.1002/cncr.26068. Epub 2011 Mar 31. PubMed PMID: 21456002.
10: 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. A phase I study of tasisulam sodium (LY573636 sodium), a novel anticancer compound in patients with refractory solid tumors. Cancer Chemother Pharmacol. 2011 Nov;68(5):1233-41. doi: 10.1007/s00280-011-1593-0. Epub 2011 Mar 23. PubMed PMID: 21431416; PubMed Central PMCID: PMC3215883.
11: Haritunians T, Gueller S, O'Kelly J, Ilaria R Jr, Koeffler HP. Novel acyl sulfonamide LY573636-sodium: effect on hematopoietic malignant cells. Oncol Rep. 2008 Nov;20(5):1237-42. PubMed PMID: 18949427; PubMed Central PMCID: PMC2659324.
