ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors Indisulam

Indisulam

Product NameIndisulam
CAS165668-41-7
MFC14H12ClN3O4S2
MW385.85
EINECS
MOL File165668-41-7.mol

Chemical Properties

Melting point	242-243 °C (decomp)(Solv: ethanol (64-17-5); water (7732-18-5))
Boiling point	668.9±65.0 °C(Predicted)
Density	1.663±0.06 g/cm3(Predicted)
storage temp.	-20°C
solubility	DMSO : 100 mg/mL (259.17 mM; Need ultrasonic)
form	powder
pka	8.14±0.30(Predicted)
color	white to beige
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)
InChIKey	SETFNECMODOHTO-UHFFFAOYSA-N
SMILES	C1(S(NC2C3=C(C=CC=2)C(Cl)=CN3)(=O)=O)=CC=C(S(N)(=O)=O)C=C1

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids
Hazard Classifications	Eye Irrit. 2 Skin Irrit. 2

Usage And Synthesis

Uses

Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15[1][2].

Definition

ChEBI: Indisulam is a chloroindole that is 3-chloro-1H-indole substituted by a [(4-sulfamoylphenyl)sulfonyl]nitrilo group at position 7. It is a carbonic anhydrase inhibitor and a potential anti-cancer agent currently in clinical development. It has a role as an EC 4.2.1.1 (carbonic anhydrase) inhibitor and an antineoplastic agent. It is a chloroindole, a sulfonamide and an organochlorine compound.

Biochem/physiol Actions

Indisulam is a carbonic anhydrase inibitor and Antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition.

in vivo

Indisulam (E7070, 12.5, 25, 50 (100) mg/kg) shows an antitumour spectrum in human cancer models^[1].

Animal Model:	Female BALB/c nu/nu mice aged 7 weeks (HCT116 colon, LX-1 lung, SW620 colon, HCT115 colon, PC-9 lung, DLD-1 colon and WiDr colon models)^[1].
Dosage:	12.5, 25, 50 (100) mg/kg.
Administration:	IV daily for 4 days.
Result:	Exhibited anti-tumor activity.

storage

Store at -20°C

References

[1] Ozawa Y, et al. E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo. Eur J Cancer. 2001 Nov;37(17):2275-82. DOI:10.1016/s0959-8049(01)00275-1
[2] Abbate F, et al. Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. Bioorg Med Chem Lett. 2004 Jan 5;14(1):217-23. DOI:10.1016/j.bmcl.2003.09.062

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