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Indisulam

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Chemical Structure| 165668-41-7 同义名 : E 7070
CAS号 : 165668-41-7
货号 : A126168
分子式 : C14H12ClN3O4S2
纯度 : 99%+
分子量 : 385.846
MDL号 : MFCD00945325
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(272.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Indisulam is an aryl sulfonamide drug with selective anticancer activity. Indisulam promotes the recruitment of RBM39 (RNA binding motif protein 39) to the CUL4-DCAF15 E3 ubiquitin ligase, leading to RBM39 polyubiquitination and proteasomal degradation[3]. Similarly to the clinically used drugs acetazolamide, methazolamide and topiramate, E7070 showed inhibition constants in the range of 15-31nM against isozymes I, II and IX, being slightly less effective as a CA IV inhibitor (K(i) of 65nM) [4]. Indisulam 500 mg m(-2) in combination with carboplatin 6 mg min ml(-1) was identified not to cause dose limiting toxicity, but a delay of re-treatment by 1 week was required regularly to allow recovery from myelosuppression[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03485950 Other Infectious Diseases Phase 2 Recruiting May 2019 United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact       iraad@mdanderson.org 收起 <<
NCT00165867 Colorectal Cancer Phase 2 Completed - France ... 展开 >> Hôpitaux Civils de Colmar Colmar, France, F- 68024 CRLC Val d'Aurelle Montpellier, France, F-34298 Centre Antoine Lacassagne Nice, France, F-06189 United Kingdom Aberdeen Royal Infirmary Aberdeen, United Kingdom, AB25 2ZN Beatson Oncology Centre Glasgow, United Kingdom, G11 6NT Cookridge Hospital Leeds, United Kingdom, LS16 6QB Leicester Royal Infirmary Leicester, United Kingdom, LE1 5WW 收起 <<
NCT00059735 Kidney Neoplasms ... 展开 >> Carcinoma, Renal Cell Adenocarcinoma, Renal Cell 收起 << Phase 2 Completed - United States, California ... 展开 >> Sacramento, California, United States, 95817 United States, New York Bronx, New York, United States, 10466 New York, New York, United States, 10021 New York, New York, United States, 10032 France Villejuif Cedex, France, 94805 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.96mL

2.59mL

1.30mL

25.92mL

5.18mL

2.59mL
参考文献

[1]Talbot DC, von Pawel J, et al. A randomized phase II pharmacokinetic and pharmacodynamic study of indisulam as second-line therapy in patients with advanced non-small cell lung cancer. Clin Cancer Res. 2007 Mar 15;13(6):1816-22.

[2]Abbate F, Casini A, et al. Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Bioorg Med Chem Lett. 2004 Jan 5;14(1):217-23.

[3]Han T, Goralski M, Gaskill N, Capota E, Kim J, Ting TC, Xie Y, Williams NS, Nijhawan D. Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15. Science. 2017 Apr 28;356(6336):eaal3755

[4]Abbate F, Casini A, Owa T, Scozzafava A, Supuran CT. Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Bioorg Med Chem Lett. 2004 Jan 5;14(1):217-23

[5]Dittrich C, Zandvliet AS, Gneist M, Huitema AD, King AA, Wanders J. A phase I and pharmacokinetic study of indisulam in combination with carboplatin. Br J Cancer. 2007 Feb 26;96(4):559-66