STX-0119
Names
Biological Activity
[Description]:
STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM[1].
[Related Catalog]:
[Target]
STAT3:74 μM (IC50, STAT3 transcription)
[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[1]. STX-0119 (10-50 μM; 24 h) reduces the expression of STAT3 target proteins[1]. Western Blot Analysis[1] Cell 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[1]. 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[1]. Animal Model: Male BALB/cA-ν/ν nude mice, SCC-3 lymphoma xenograft model[1] Dosage: 160 mg/kg Administration: Oral gavage, daily for 4 days Result: Suppressed the growth of SCC-3 cells significantly on the fourth day.
Chemical & Physical Properties
[ Molecular Formula ]:
C22H14N4O3
[ Molecular Weight ]:
382.37200
[ Exact Mass ]:
382.10700
[ PSA ]:
94.05000
[ LogP ]:
4.87010
[ Storage condition ]:
2-8°C