Indisulam

For research use only.

Catalog No.S9742 Synonyms: E7070

Indisulam Chemical Structure

CAS No. 165668-41-7

Indisulam (E7070), a sulfonamide anticancer agent, is a potent carbonic anhydrase (CA) inhibitor that inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Indisulam suppresses the expression of cyclin E and phosphorylation of CDK2, both of which are essential for the G1 to S transition.

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Biological Activity

Description Indisulam (E7070), a sulfonamide anticancer agent, is a potent carbonic anhydrase (CA) inhibitor that inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Indisulam suppresses the expression of cyclin E and phosphorylation of CDK2, both of which are essential for the G1 to S transition.
Targets
CA [1]
()
cyclin E [1]
()
CDK2 [1]
()
In vitro

Following treatment with E7070, the cell cycle progression of P388 murine leukaemia cells is disturbed in the G1 phase. The cell-killing effect on human colon cancer HCT116 cells is found to be time-dependent. In the panel of 42 human tumour cell lines, E7070 shows an antitumour spectrum that is distinct from those of other anticancer drugs used in clinic.[2]

In vivo

Animal tests using human tumour xenograft models demonstrates that E7070 can cause not only tumour growth suppression, but also tumour regression in three of five colorectal and two of two lung cancers. In the HCT116 xenograft model, E7070 is shown to be superior to 5-FU, MMC and CPT-11 (irinotecan). Furthermore, complete regression of advanced LX-1 tumours is observed in 80% of E7070-treated mice.[2]

Protocol

Cell Research:

[2]

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  • Cell lines: P388 cells, HCT116 cells
  • Concentrations: 0.14 μg/ml, 0.41 μg/ml, 1.2 μg/ml, 3.7 μg/ml, 11 μg/ml, 33 μg/ml, 100 μg/ml
  • Incubation Time: 12 h, 24 h, 48 h
  • Method:

    P388 cells are seeded at 1.25–10×105 cells/well in 24-well plates. After E7070 is added to each well, the cells are incubated for 12, 24 or 48 h. At the indicated time points, the cells are fixed in 70% ethanol at 4 ℃ for 1 h, stained with propidium iodide (50 μg/ml), and then analysed for DNA content by quantitation of red fluorescence in a flow cytometer.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: 7-week-old female BALB/c nu/nu mice
  • Dosages: 12.5 mg/kg, 25 mg/kg, 50 mg/kg, 100 mg/kg
  • Administration: IV
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 77 mg/mL (199.55 mM)
Water Insoluble
Ethanol '10 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 385.85
Formula

C14H12ClN3O4S2

CAS No. 165668-41-7
Storage powder
in solvent
Synonyms E7070

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00165594 Terminated Drug: E7070 Gastric Cancer Eisai Co. Ltd.|Eisai Inc. February 2005 Phase 1|Phase 2
NCT00165854 Completed Drug: E7070 Colorectal Cancer (CRC) Eisai Limited|Eisai Inc. March 2003 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Carbonic Anhydrase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID