851095-32-4

Usage

Uses

Used in Oncology:
STX-0119 is used as a cancer therapeutic agent for targeting STAT3, a protein that plays a crucial role in the development and progression of various cancers, including Glioblastoma multiforme. By inhibiting STAT3, STX-0119 aims to suppress tumor growth and improve patient outcomes.
Used in Drug Development:
STX-0119 is used as a drug target in the development of novel cancer therapies. Its ability to inhibit STAT3 makes it a valuable candidate for the creation of new drugs that can effectively combat cancer cells and enhance the efficacy of existing treatments.

Upstream product

• 1236056-73-7 C₂₂H₁₆N₄O₃S 
• 7659-06-5 5-furan-2-yl-[1,3,4]oxadiazol-2-ylamine 
• 132-60-5 cinchophen 
• 59661-86-8 2-phenylquinoline-4-carbonyl chloride 

Downstream Products

• 1204212-53-2 N-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-N-methyl-2-phenyl-4-quinolinecarboxamide 

Relevant academic research and scientific papers

STAT3 INHIBITOR CONTAINING QUINOLINECARBOXAMIDE DERIVATIVE AS ACTIVE INGREDIENT

The present invention provides a STAT3 inhibitor containing as an active ingredient, a quinolinecarboxamide derivative represented by the formula (I) (in the formula, W represents a bond or an alkylene chain; X represents O, S, or NR34; and Rs

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.