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/ Indisulam

Indisulam {[allProObj[0].p_purity_real_show]}

货号：A126168 同义名： E 7070

Indisulam is a carbonic anhydrase inhbitor and a synthetic sulfonamide targeting the G1 phase of the cell cycle.

Indisulam 化学结构 CAS号：165668-41-7
Indisulam 化学结构
CAS号：165668-41-7
Indisulam 3D分子结构
CAS号：165668-41-7
Indisulam 化学结构 CAS号：165668-41-7
Indisulam 3D分子结构 CAS号：165668-41-7
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Indisulam 纯度/质量文件 产品仅供科研

货号：A126168 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Carbonic Anhydrase ↓ Carbonic Anhydrase I ↓ Carbonic Anhydrase II ↓ Carbonic Anhydrase IV ↓ Carbonic Anhydrase IX ↓ Carbonic Anhydrase XII ↓ 其他靶点 纯度
Topiramate ✔ Calcium Channel 98%
Dichlorphenamide ✔ 98%
Mafenide Acetate ✔ 98%
Benzenesulphonamide ✔ 98%
Dorzolamide HCl +

Carbonic anhydrase I, Ki: 6000 nM

 		++++

Carbonic anhydrase II, Ki: 1.9 nM

 		+++

Carbonic anhydrase IV, Ki: 31 nM

 		98%
Methazolamide ++

hCAI, Ki: 50 nM

 		+++

hCAII, Ki: 14 nM

 		++

bCAIV, Ki: 36 nM

 		98%
Tioxolone +

CAI, Ki: 91 nM

 		98%
U-104 ++

CAIX, Ki: 45.1 nM

 		++++

CAXII, Ki: 4.5 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Indisulam 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].

Indisulam 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 <<

Indisulam 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

Indisulam 实验方案

计算器
存储液制备 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

Indisulam 技术信息

CAS号165668-41-7
分子式C14H12ClN3O4S2
分子量 385.846
别名 E 7070
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

Tags: Indisulam | 165668-41-7 | E 7070 | E7070 | E-7070 | PROTAC | Metabolic Enzyme/Protease | Molecular Glues | Carbonic Anhydrase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Indisulam 纯度/质量文件 | Indisulam 亚型比较 | Indisulam 生物活性 | Indisulam 临床数据 | Indisulam 参考文献 | Indisulam 实验方案 | Indisulam 技术信息

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