Home Metabolism Carbonic Anhydrase inhibitor - CDK inhibitor Indisulam For research use only.

Indisulam

Synonyms: E7070

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.

Indisulam Chemical Structure

Indisulam Chemical Structure

CAS: 165668-41-7

Selleck's Indisulam has been cited by 1 publication

Purity & Quality Control

Batch: S974201 DMSO] 77 mg/mL] false] Ethanol] 10 mg/mL] false] Water] Insoluble] false Purity: 99.85%
99.85

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00165594 Terminated
Gastric Cancer
Eisai Co. Ltd.|Eisai Inc.
 February 2005 Phase 1|Phase 2
NCT00165854 Completed
Colorectal Cancer (CRC)
Eisai Limited|Eisai Inc.
 March 2003 Phase 2

Chemical Information & Solubility

Molecular Weight 385.85 Formula

C14H12ClN3O4S2
CAS No. 165668-41-7 SDF --
Smiles N[S](=O)(=O)C1=CC=C(C=C1)[S](=O)(=O)NC2=C3[NH]C=C(Cl)C3=CC=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 77 mg/mL ( (199.55 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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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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