Indisulam

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.

Product information

CAS Number: 165668-41-7

Molecular Weight: 385.85

Formula: C14H12ClN3O4S2

Synonym:

E7070

Chemical Name: N-(3-Chloro-1H-indol-7-yl)-1,4-benzenedisulfonamide

Smiles: NS(=O)(=O)C1=CC=C(C=C1)S(=O)(=O)NC1=CC=CC2=C1NC=C2Cl

InChiKey: SETFNECMODOHTO-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO 77 mg/mL (199.56 mM) Ethanol 10 mg/mL (25.92 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

References:

1. Francesco Abbate, et al. Bioorg Med Chem Lett. 2004 Jan 5;14(1):217-23.
2. Y Ozawa, et al. Eur J Cancer. 2001 Nov;37(17):2275-82.

Products are for research use only. Not for human use.