Indisulam Inhibitor CAS No. 165668-41-7

Cat. No.	Name	Size	Price
KI1488	Indisulam	10 mg	$330
	Indisulam	25 mg	$530
	Indisulam	50 mg	$730

Chemical Characteristic

Product Name	Indisulam
Synonyms	E7070, ER-35744, D04522
CAS No.	165668-41-7
Molecular Weight	385.84
Formula	C₁₄H₁₂ClN₃O₄S₂
Chemical Name	N-(3-Chloro-1H-indol-7-yl)-1,4-benzenedisulfonamide
Smiles	c1(ccc(cc1)S(=O)(=O)N)S(=O)(=O)Nc1cccc2c(c[nH]c12)Cl
Chemical Structure
Documents	CNMR HNMR

Biological activities

Indisulam is a potent carbonic anhydrase inhbitor and tubulin polymerization inhibitor. Continuous exposure of indisulam inhibits cell proliferation with IC50 values of 0.1-4.4 µg/mL against different tumors including HCT116, KB, colon 38 and P388 cells.^[1] Indisulam suppresses the expression of cyclin E and phosphorylation of CDK2 and provokes cell-cycle arrest in the G1 phase. Furthermore, indisulam disrupts cell-cycle progression at multiple points, including both the G1/S and the G2/M transition, in A549 human NSCLC.^[2]Intraperitoneal or intravenous administration of indisulam produces not only growth suppression but also a significant reduction in tumor size of HCT116 xenografts at dose of 25 and 50 mg/kg/day for 4 days.^[2] Moreover, in the HCT116 xenograft model, the antitumor activity of indisulam is superior to 5-FU, MMC and CPT-11 (irinotecan). Complete regression of advanced LX-1 tumours is observed in 80% of indisulam-treated mice.^[3]

Protocols

In vivo: Indisulam is dissolved at appropriate concentrations in 3.5% DMSO and 6.5% Tween 80 in saline.^[3]

References

[1] Owa T, et al. Discovery of novel antitumor sulfonamides targeting G1 phase of the cell cycle. J Med Chem. 1999, 42(19): 3789-3799. [2] Supuran CT, et al. Indisulam: an anticancer sulfonamide in clinical development. Expert Opin Investig Drugs. 2003, 12(2): 283-287. [3] Ozawa Y, et al. E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo. Eur J Cancer. 2001, 37(17): 2275-2282.

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