|4-(N-(4-环己基苄基)-2-(2,3,4,5,6-五氟-N-甲基苯基磺酰胺基)乙酰氨基)苯甲酸|CsnPharm

CAS No.: 1456632-40-8

SH-4-54 Catalog No. CSN17881

SH-4-54 is a potent, small molecule, nonphosphorylated STAT3 inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

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

Kd:300nM STAT5

Kd:464nM
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. SH-4-54 is a selective STAT3 inhibitor with KD value of 300nM (measured by binding affinity). Treatment with SH-4-54 at concentration ranging in 0.5-5μM dose-dependently inhibited the level of p-STAT3-Y705, but not p-STAT3-S727, and its downstream target genes Bcl-xL and Cyclin D1 in 147EF cells, decrease of which can promote apoptosis of cells. SH-4-54 exhibited BBB permeability. Administration of 10mg/kg SH-4-54, i.p., on 4 days on/3 days off schedule, significantly decreased tumor growth with downregulated p-STAT3 in mice orthotopically xenografted with BT73.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human 127EF cells	-	Cytotoxic assay	3 days	Cytotoxicity against human 127EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=66 nM	24900612
human 147EF cells	-	Function assay	2-72 h	Inhibition of STAT3 in human 147EF cells assessed as reduction of phosphorylated cyclin D1 level after 2 to 72 hrs by Western blotting analysis	24900612
human 25EF cells	-	Cytotoxic assay	3 days	Cytotoxicity against human 25EF cells assessed as cell viability after 3 days by Alamar Blue assay, IC50=0.234 μM	24900612

更多
动物研究
剂量
Mice: 3 mg/kg - 6 mg/kg^[3] (p.o.); 10 mg/kg^[4] (i.v.), 20 mg/kg^[4] (i.p.)

给药途径
p.o., i.v., i.p.

动物研究
剂量	Mice: 3 mg/kg - 6 mg/kg^[3] (p.o.); 10 mg/kg^[4] (i.v.), 20 mg/kg^[4] (i.p.)
给药途径	p.o., i.v., 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
- 1.6378 mL
- 8.1888 mL
- 16.3775 mL
- 5 mM
- 0.3276 mL
- 1.6378 mL
- 3.2755 mL
- 10 mM
- 0.1638 mL
- 0.8189 mL
- 1.6378 mL

技术信息

CAS号

1456632-40-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H27F5N2O5S

运输

蓝冰

分子量

610.59

别名

溶解度

DMSO	100.0 mg/mL (163.8 mM)
Water	Insoluble
Ethanol	50.0 mg/mL (81.9 mM) warming

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

靶点	Description	IC50
STAT3		Kd:300nM
STAT5		Kd:464nM

SH-4-54 Catalog No. CSN17881

靶点选择性

请登录您的专属账户

确认信息