Indisulam

Catalog No.S9742 Batch:S974201

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Technical Data

Formula

C14H12ClN3O4S2
Molecular Weight 385.85 CAS No. 165668-41-7
Solubility (25°C)* In vitro DMSO 77 mg/mL (199.55 mM)
Ethanol 10 mg/mL (25.91 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.64mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.85mg/ml Taking the 1 mL working solution as an example, add 50 μL of 77 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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. Furthermore, complete regression of advanced LX-1 tumours is observed in 80% of E7070-treated mice.[2]

Protocol (from reference)

Cell Assay:

[2]
  • 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.
Animal Study:

[2]
  • 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

Selleck's Indisulam has been cited by 2 publications

YAP/TAZ interacts with RBM39 to confer resistance against indisulam [ Oncogenesis, 2024, 13(1):25] PubMed: 39004623
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9] PubMed: 35868306

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.