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STX-0119
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
STX-0119图片
CAS NO:851095-32-4

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。
生物活性

STX-0119 is a selective, orally activeSTAT3dimerization inhibitor. STX-0119 inhibitsSTAT3transcription with anIC50of 74 μM[1].

IC50& Target[1]

STAT3

74 μM (IC50, STAT3 transcription)

体外研究
(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.
体内研究
(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.
分子量

382.37

性状

Solid

Formula

C22H14N4O3

CAS 号

851095-32-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

 
 
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