|2-羟基--4-(2-(甲苯磺酰氧基)乙酰氨基)苯甲酸|CsnPharm

CAS No.: 501919-59-1

NSC 74859 Catalog No. CSN15990

Synonyms: NSC 74859NSC 74859NSC 74859NSC 74859NSC 74859;S3I 20;S3I-201

S3I-201 shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM, and low activity towards STAT1 and STAT5.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 STAT3

IC50:86μM
描述STAT3, the protein most linked to tumorigenesis in STAT family and regarded as a target for cancer therapy, is constitutively activated in most human solid tumors and is involved in the proliferation, angiogenesis, immune evasion, and anti-apoptosis of cancer cells. S3I-201 is a selective inhibitor of STAT3 with IC50 value of 86μM for inhibition of Stat3 DNA-binding activity. Treatment with S3I-201 at concentration of 100μM for 24h led to obvious inhibition of STAT3-Tyr705 phosphorylation in NIH 3T3/v-Src fibroblasts. The disruption of STAT3 dimerization and suppression on Stat3-dependent transcriptional activity by S3I-201 could also be observed in EMSA analysis and luciferase assay, respectively. Significant cell growth inhibition by 100μM S3I-201 can be observed in both of anchorage-dependent and -independent cells containing persistently active Stat3, including NIH 3T3/v-Src, MDA-MB-435, MDA-MB-231, or MDA-MB-468, but not in cells aberrant Stat3 activity, including NIH
3T3 and MDA-MB-453, due to the apoptosis accompanied with inhibited cyclin D1, Bcl-xL, and survivin expression. Intravenous injection with S3I-201 at dose of 5mg/kg, every 2 or every 3 days for 16 days significant inhibited tumor growth in MDA-MB-231 tumor-bearing mice.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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动物研究
剂量
Mice: 5 mg/kg^[3] (i.p.), 20 mg/kg^[4] (i.p.)

给药途径
i.p.

动物研究
剂量	Mice: 5 mg/kg^[3] (i.p.), 20 mg/kg^[4] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7370 mL
- 13.6852 mL
- 27.3704 mL
- 5 mM
- 0.5474 mL
- 2.7370 mL
- 5.4741 mL
- 10 mM
- 0.2737 mL
- 1.3685 mL
- 2.7370 mL

技术信息

CAS号

501919-59-1

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H15NO7S

运输

蓝冰

分子量

365.36

别名

NSC 74859NSC 74859NSC 74859NSC 74859NSC 74859;S3I 20;S3I-201

溶解度

DMSO	73.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+corn oil

3 mg/mL

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NSC 74859 Catalog No. CSN15990

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