NSC 74859 (S3I-201) acts as a selective inhibitor of Stat3, demonstrating an IC50 of 86 μM[1].
NSC 74859 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
A459
100 nM
Apoptosis Assay
24 h
induces cell apoptosis co-treated with BEZ235
24472538
BT474R
50 μM
Function Assay
10-60 d
inhibits STAT3 activity
25327561
GC
50-125 μM
Growth Inhibition Assay
72 h
attenuates the cell growth in a dose-dependent manner
25774503
GH3
50-125 μM
Growth Inhibition Assay
72 h
attenuates the cell growth in a dose-dependent manner
25774503
NSC 74859 动物研究
Animal study
Mice bearing human breast (MDA-MB-231) tumors receive intravenous injections of NSC 74859 (S3I-201) or a vehicle solution every two or three days over a period of two weeks, with tumor sizes measured every 2-3 days. In contrast to the control group receiving vehicle solution, whose tumors continue to grow, mice treated with S3I-201 exhibit significant inhibition of tumor growth. Further observations post-treatment cessation reveal no signs of tumor regrowth, indicating the potential for a lasting impact of S3I-201 on inhibiting tumor growth[1].In comparison to control tumors treated with vehicle solution (n=15), which exhibited continuous growth, S3I-201 treatment on somatotroph tumor xenografts (n=15) markedly reduces tumor growth throughout the study period. Tumors from NSC 74859-treated rats are notably smaller than those in the untreated group (220±16 mm3 vs. 287±16 mm3, P<0.01) as soon as five days following the injection of NSC 74859. By the fifteenth day post-treatment, the average tumor volume in NSC 74859-treated rats is only 64% of that in control animals (449±40 mm3 vs. 708±83 mm3, P<0.01). The experiment concludes with the rats being euthanized and the tumors collected 15 days after beginning treatment, revealing an average tumor weight in NSC 74859-treated rats of 78±8 mg, compared to 114±13 mg in tumors from control rats, a 32% reduction (P<0.05)[3].
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