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/ Indisulam

Indisulam {[allProObj[0].p_purity_real_show]}

货号：A126168 同义名： E 7070

Indisulam是一种碳酸酐酶抑制剂，也是一种合成磺胺类化合物，靶向细胞周期的G1期。

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:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
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 细胞实验

Cell Line
Concentration Treated Time Description References
LP-1 20 μM 48 hours Inhibited MM cell proliferation and induced apoptosis Blood Adv. 2025 Apr 22;9(8):1991-2005
MM.1S 20 μM 48 hours Inhibited MM cell proliferation and induced apoptosis Blood Adv. 2025 Apr 22;9(8):1991-2005
H929 20 μM 48 hours Inhibited MM cell proliferation and induced apoptosis Blood Adv. 2025 Apr 22;9(8):1991-2005
IMR-32 5 µM 16 h To assess the impact of Indisulam on cell cycle and metabolism-related proteins. Results showed significant decreases in CDK4 and TYMS protein levels. Nat Commun. 2022 Mar 16;13(1):1380
KELLY 1 or 10 µM 0.5–24 h To validate RBM39 degradation induced by Indisulam. Western blot analysis confirmed RBM39 degradation. Nat Commun. 2022 Mar 16;13(1):1380
IMR-32 5 µM 6 h To evaluate the selective degradation of RBM39 by Indisulam. Results showed a significant reduction in RBM39 abundance (~9-fold). Nat Commun. 2022 Mar 16;13(1):1380
B16-F10 cells 1μM 96 hours Evaluate the effect of Indisulam on tumor cell growth, results showed inhibition of cell growth after drug treatment Cell. 2021 Jul 22;184(15):4032-4047. e31
BE2C 250 nM 72 hours To evaluate the effect of Indisulam on RBM39 degradation, results showed that Indisulam induced dose-dependent reduction of RBM39. Sci Adv. 2021 Nov 19;7(47):eabj5405
HuCCT1 cells 10 μM 48 hours To evaluate the effect of Indisulam on CCA cell growth, results showed that Indisulam significantly inhibited cell proliferation and colony formation ability Cell Mol Gastroenterol Hepatol. 2025;19(1):101404
CCLP1 cells 10 μM 48 hours To evaluate the effect of Indisulam on CCA cell growth, results showed that Indisulam significantly inhibited cell proliferation and colony formation ability Cell Mol Gastroenterol Hepatol. 2025;19(1):101404
Jurkat 5 μM 48 hours To evaluate the antitumor effects of Indisulam on T-ALL cells. Results showed that Indisulam significantly inhibited cell proliferation, promoted apoptosis, and interfered with cell cycle progression. J Exp Clin Cancer Res. 2024 Jul 24;43(1):205
J.gamma1 1 μM 48 hours To evaluate the antitumor effects of Indisulam on T-ALL cells. Results showed that Indisulam significantly inhibited cell proliferation, promoted apoptosis, and interfered with cell cycle progression. J Exp Clin Cancer Res. 2024 Jul 24;43(1):205

Indisulam 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Neuroblastoma xenograft model Intravenous injection 25 mg/kg 5 days on and 2 days off for two weeks To evaluate the antitumor effect of Indisulam in vivo, results showed that Indisulam induced an initial complete response in all models, but the time to relapse in neuroblastoma was significantly longer compared to other models. Sci Adv. 2021 Nov 19;7(47):eabj5405
NSG immunodeficient mice Subcutaneously injected with SUIT2 or A549 cells Retro-orbital injection 40 mg/kg 8 days for SUIT2 cells and 5 days for A549 cells Indisulam significantly inhibited tumor growth of SUIT2 and A549 cells, with a more pronounced effect on SUIT2 cells. Nat Commun. 2021 Jul 13;12(1):4288
NCr Foxnnu mice IMR-32 xenograft model Intravenous 25 mg/kg 8 consecutive days To evaluate the antitumor efficacy of Indisulam in vivo. Results showed complete tumor regression without relapse. Nat Commun. 2022 Mar 16;13(1):1380
Mice B16-F10 tumor model Intravenous injection 25 mg/kg 5 days per week, continuous treatment Evaluate the inhibitory effect of Indisulam on tumor growth, results showed significant tumor growth inhibition and enhanced efficacy of immune checkpoint blockade therapy Cell. 2021 Jul 22;184(15):4032-4047. e31
NOD/SCID mice Subcutaneous xenograft model Intraperitoneal injection 15 mg/kg 3 times per week for a total of 7 times To evaluate the inhibitory effect of Indisulam alone or in combination with MS177 on CCA tumor growth, results showed that combination therapy significantly inhibited tumor growth Cell Mol Gastroenterol Hepatol. 2025;19(1):101404
NOD scid gamma (NSG) mice T-ALL xenograft model Intraperitoneal injection 12.5 mg/kg Once daily for 5 days on and 2 days off, repeated twice To evaluate the antitumor effects of Indisulam on T-ALL in vivo. Results showed that Indisulam significantly inhibited tumor growth, prolonged survival, and had no significant toxic side effects. J Exp Clin Cancer Res. 2024 Jul 24;43(1):205
NOG mice Subcutaneous H929 tumor model Intraperitoneal injection 10 mg/kg 9 consecutive days Significantly reduced tumor volume Blood Adv. 2025 Apr 22;9(8):1991-2005

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 385.85
SMILES Code O=S(C1=CC=C(S(=O)(N)=O)C=C1)(NC2=CC=CC3=C2NC=C3Cl)=O
MDL No. MFCD00945325
别名 E 7070
运输蓝冰
InChI Key SETFNECMODOHTO-UHFFFAOYSA-N
Pubchem ID 216468
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

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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