STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM[1].
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. |
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. |
[1]. Matsuno K, et al. Identification of a New Series of STAT3 Inhibitors by Virtual Screening. ACS Med Chem Lett. 2010 Jul 13;1(8):371-5.