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Indisulam (E7070) Carbonic Anhydrase inhibitor

Cat.No.S9742

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 (E7070) Carbonic Anhydrase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 385.85

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 77 mg/mL (199.55 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 385.85 Formula

C14H12ClN3O4S2

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 165668-41-7 -- Storage of Stock Solutions

Synonyms E7070 Smiles N[S](=O)(=O)C1=CC=C(C=C1)[S](=O)(=O)NC2=C3[NH]C=C(Cl)C3=CC=C2

Mechanism of Action

Targets/IC50/Ki
CA
cyclin E
CDK2
In vitro

Following treatment with this compound, 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, it shows an antitumour spectrum that is distinct from those of other anticancer drugs used in clinic.

In vivo

Animal tests using human tumour xenograft models demonstrates that this compound 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, it 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.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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