865287-85-0

Basic information

• Product Name: 2-phenyl-N-[5-(2-thienyl)-1,3,4-oxadiazol-2-yl]-4-quinolinecarboxamide
• CAS NO: 865287-85-0
• Molecular Weight: 398.445
• Mol File: 865287-85-0.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: 2-phenyl-N-[5-(2-thienyl)-1,3,4-oxadiazol-2-yl]-4-quinolinecarboxamide(CAS DataBase Reference)
• NIST Chemistry Reference: 2-phenyl-N-[5-(2-thienyl)-1,3,4-oxadiazol-2-yl]-4-quinolinecarboxamide(865287-85-0)
• EPA Substance Registry System: 2-phenyl-N-[5-(2-thienyl)-1,3,4-oxadiazol-2-yl]-4-quinolinecarboxamide(865287-85-0)

Safety Data

• Hazardous Substances Data: 865287-85-0(Hazardous Substances Data)

Upstream product

• 27049-71-4 5-(thiophen-2-yl)-1,3,4-oxadiazol-2-amine 
• 132-60-5 cinchophen 

Relevant articles and documents

Identification of a new series of STAT3 inhibitors by virtual screening

The signal transducer and activator of transcription 3 (STAT3) is considered to be an attractive therapeutic target for oncology drug development. We identified a N-[2-(1,3,4-oxadiazolyl)]-4-quinolinecarboxamide derivative, STX-0119, as a novel STAT3 dimerization inhibitor by a virtual screen using a customized version of the DOCK4 program with the crystal structure of STAT3. In addition, we used in vitro cell-based assays such as the luciferase reporter gene assay and the fluorescence resonance energy transfer-based STAT3 dimerization assay. STX-0119 selectively abrogated the DNA binding activity of STAT3 and suppressed the expression of STAT3-regulated oncoproteins such as c-myc and survivin in cancer cells. In contrast, a truncated inactive analogue, STX-0872, did not exhibit those activities. Oral administration of STX-0119 effectively abrogated the growth of human lymphoma cells in a SCC-3 subcutaneous xenograft model without visible toxicity. Structure-activity relationships of STX-0119 derivatives were investigated using the docking model of the STAT3-SH2 domain/STX-0119.