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| 10mg |
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| 25mg |
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| 50mg |
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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 |
Indisulam is a chloroindole that is 3-chloro-1H-indole substituted by a [(4-sulfamoylphenyl)sulfonyl]nitrilo group at position 7. It is a carbonic anhydrase inhibitor and a potential anti-cancer agent currently in clinical development. It has a role as an EC 4.2.1.1 (carbonic anhydrase) inhibitor and an antineoplastic agent. It is a chloroindole, a sulfonamide and an organochlorine compound.
Indisulam is a novel sulfonamide compound with potential antineoplastic activity. Indisulam inhibits cyclin-dependent kinases (CDK), which regulate cell cycle progression and are usually over-expressed in cancerous cells. Inhibition of CDK results in G1/S phase arrest of the cell cycle, and may lead to induction of apoptosis and inhibition of tumor cell proliferation. In addition, indisulam also inhibits carbonic anhydrases (CA), especially isoforms IX and XII that are involved in aqueous humor production and are highly overexpressed in some types of cancers. Inhibition of CA IX and XII results in interference with ion exchange and pH in hypoxic tumor tissue and preventing chemoresistance to weakly basic antineoplastic agents. Drug Indication Investigated for use/treatment in lung cancer. Mechanism of Action E7070 is a novel sulfonamide antitumoragent that exhibits potent antitumoractivity in vitro and in vivo. This compound affects cell cycleprogression in human tumor cells |
| Molecular Formula |
C14H12CLN3O4S2
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|---|---|
| Molecular Weight |
385.8458
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| Exact Mass |
384.995
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| 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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