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。
产品描述
STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM.
体外活性
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[1].
体内活性
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[1].
Cas No.
851095-32-4
分子式
C22H14N4O3
分子量
382.37
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years