LY-295501

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C15H12Cl2N2O4S
Molecular Weight	387.238
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

ClC1=C(Cl)C=C(NC(=O)NS(=O)(=O)C2=CC=C3OCCC3=C2)C=C1

InChI

InChIKey=VAMFSFIPDOODFH-UHFFFAOYSA-N

InChI=1S/C15H12Cl2N2O4S/c16-12-3-1-10(8-13(12)17)18-15(20)19-24(21,22)11-2-4-14-9(7-11)5-6-23-14/h1-4,7-8H,5-6H2,(H2,18,19,20)

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Description
Sources: https://adisinsight.springer.com/drugs/800003361 | https://www.ncbi.nlm.nih.gov/pubmed/7795279 | https://www.ncbi.nlm.nih.gov/pubmed/14654534

LY 295501 (ILX 295501) is a diarylsulfonylurea with potential antitumor activity both in vivo and in vitro. It was being developed for the treatment of solid malignancies. LY 295501 development has been discontinued.

Originator

Approval Year

PubMed

Title	Date	PubMed
A phase I and pharmacokinetic study of ILX-295501, an oral diarylsulfonylurea, on a weekly for 3 weeks every 4-week schedule in patients with advanced solid malignancies.	2003-11-15	14654534
Significant activity of a novel cytotoxic agent, LY295501, against a wide range of tumors in the human tumor cloning system.	1999-03	10327037
Studies on the mechanism of sulofenur and LY295501 toxicity: effect on the regulation of cytosolic calcium in relation to cytotoxicity in normal and tumorigenic rat kidney cell lines.	1995-10-20	7585481
Efficacy of sulofenur and a second generation diarylsulfonylurea, N-[5-(2,3-dihydrobenzofuryl)sulfonyl]-N'-(3,4-dichlorophenyl)urea (LY295501), against colon adenocarcinoma xenografts.	1995-04	7795279

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose for Phase II studies of the oral DSU ILX-295501 administered weekly for 3 weeks every 4 weeks is 1000 mg/m(2)/day for both minimally pretreated and HP patients. The characteristics of the myelosuppressive effects of ILX-295501, the paucity of severe nonhematological toxicities, and preliminary antitumor activity warrant disease-directed evaluations of ILX-295501.

Route of Administration: Oral

In Vitro Use Guide

Treatment of NRK-52E (normal) and H/1.2-NRK-52E (Harvey-ras transfected NRK-52E) rat kidney epithelial-like cells with LY295501 (15.6 microM-1000 microM) resulted in concentration- and time-dependent cell killing.

Name

Type

Language

ILX-295501

Preferred Name

English

LY-295501

Common Name

English

5-BENZOFURANSULFONAMIDE, N-(((3,4-DICHLOROPHENYL)AMINO)CARBONYL)-2,3-DIHYDRO-

Systematic Name

English

LY295501

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C2186