STX-0119

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

STX-0119 是一种选择性的、具有口服活性的 STAT3 二聚抑制剂。STX-0119 抑制 STAT3 转录，IC50 为 74 μM。

STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM.

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.Western Blot Analysis 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.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.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.

——

JAK/STAT Signaling

STAT

STAT

——

——

851095-32-4

382.37

C22H14N4O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 13.33 mg/mL (34.86 mM; 超声助溶 (<60°C)

C(NC=1OC(=NN1)C2=CC=CO2)(=O)C=3C4=C(N=C(C3)C5=CC=CC=C5)C=CC=C4

——

(-20℃)

With Ice Pack

≥ 2 years