Indisulam

Catalog No.S9742 Batch:S974201

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
* <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.)

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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 (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

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

References

Selleck's Indisulam has been cited by 1 publication

Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9]	PubMed: 35868306

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
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