STX-0119

STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC 50 of 74 μM In Vitro STX-0119 (10-50 μM; 24 h) inhibits STAT3 dimerization through a direct interaction with the STAT3 protein and not via the modulation of upstream regulators such as JAK in HEK293 and MDA-MB-468 cells. STX-0119 (10-50 μM; 24 h) reduces the expression of STAT3 target proteins. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MDA-MB-468 cells Concentration: 10, 20 and 50 μM Incubation Time: 24 h Result: Reduced the expression of STAT3 target proteins, namely, c-myc, cyclin D1, and survivin, in a concentration-dependent manner. Did not suppress the expression of those STAT3-regulated oncoproteins. In Vivo STX-0119 (160 mg/kg; oral gavage; daily for 4 days) inhibits SCC-3 tumor growth in mice . The plasma concentration of STX-0119 (160 mg/kg; oral gavage) is maintained at >100 μg/mL (>260 μM), even at 8 h after administration . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male BALB/cA-ν/ν nude mice, SCC-3 lymphoma xenograft model Dosage: 160 mg/kg Administration: Oral gavage, daily for 4 days Result: Suppressed the growth of SCC-3 cells significantly on the fourth day. Form:Solid IC50& Target:STAT3 74 μM (IC 50 , STAT3 transcription)

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