| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
Indisulam (formerly E-7070; ER-35744; D-04522), a synthetic aryl sulfonamide, is a potent CAI-carbonic anhydrase inhibitor with potential anticancer activity. It is a multi-targeted cell cycle inhibitor and also a G1-targeting agent that can cause a blockade in the G1/S transition.
| ln Vitro |
Indisulam (E7070, 0–50 μg/mL, 12-48 hours) perturbs the G1 phase of the cell cycle in a time- and dose-dependent manner, which may result in cell death [1].
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|---|---|
| ln Vivo |
In human cancer models, indisulam (E7070, 12.5, 25, 50, 100 mg/kg) demonstrates an antitumor spectrum [1].
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| Cell Assay |
Cell cycle analysis [1]
Cell Types: P388 mouse leukemia cells. Tested Concentrations: 0-50 μg/ml. Incubation Duration: 12-48 hrs (hours). Experimental Results: P388 cells accumulated in G1 phase. |
| Animal Protocol |
Animal/Disease Models: 7weeks old female BALB/c nu/nu (nude) mice (HCT116 colon, LX-1 lung, SW620 colon, HCT115 colon, PC-9 lung, DLD-1 colon and WiDr colon models) [1].
Doses: 12.5, 25, 50 (100) mg/kg. Doses: intravenous (iv) (iv)injection daily for 4 days. Experimental Results: demonstrated anti-tumor activity. |
| References |
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| Additional Infomation |
Indesulam is a chloroindole compound with the structure 3-chloro-1H-indole, substituted at position 7 with a [(4-aminosulfonylphenyl)sulfonyl]nitrile group. It is a carbonic anhydrase inhibitor and a potential anticancer drug currently under clinical development. It functions as an EC 4.2.1.1 (carbonic anhydrase) inhibitor and an antitumor drug. It is a chloroindole, sulfonamide, and organochlorine compound. Indesulam is a novel sulfonamide compound with potential antitumor activity. Indesulam inhibits cyclin-dependent kinase (CDK), which regulates cell cycle progression and is typically overexpressed in cancer cells. Inhibition of CDK can lead to G1/S phase arrest of the cell cycle and may induce apoptosis and inhibit tumor cell proliferation. Furthermore, indolesulfonamides can also inhibit carbonic anhydrase (CA), particularly isoenzymes IX and XII involved in aqueous humor production, both of which are highly overexpressed in certain types of cancer. Inhibition of CA IX and XII can interfere with ion exchange and pH in hypoxic tumor tissues, thereby preventing resistance to weakly basic antitumor drugs.
Drug Indications It has been studied for the treatment of lung cancer. Mechanism of Action E7070 is a novel sulfonamide antitumor drug that exhibits potent antitumor activity both in vitro and in vivo. This compound can affect the cell cycle progression of human tumor cells. |
| Molecular Formula |
C14H12CLN3O4S2
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|---|---|
| Molecular Weight |
385.8458
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| Exact Mass |
384.995
|
| CAS # |
165668-41-7
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| PubChem CID |
216468
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| Appearance |
White to pink solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
668.9±65.0 °C at 760 mmHg
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| Flash Point |
358.4±34.3 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.731
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| LogP |
2.08
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
651
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SETFNECMODOHTO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H12ClN3O4S2/c15-12-8-17-14-11(12)2-1-3-13(14)18-24(21,22)10-6-4-9(5-7-10)23(16,19)20/h1-8,17-18H,(H2,16,19,20)
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| Chemical Name |
N-(3-Chloro-1H-indol-7-yl)-1,4-benzenedisulfonamide
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| Synonyms |
E7070; ER-35744; E 7070; ER 35744; E-7070; ER35744; D04522
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~259.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.17 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5917 mL | 12.9584 mL | 25.9168 mL | |
| 5 mM | 0.5183 mL | 2.5917 mL | 5.1834 mL | |
| 10 mM | 0.2592 mL | 1.2958 mL | 2.5917 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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