同义名 :	-
	CAS号 :	328998-53-4
	货号 :	A194870
	分子式 :	C23H16ClNO2
	纯度 :	99%
	分子量 :	373.83
	MDL号 :	MFCD01534890
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性
描述	Signal transducers and activators of transcription 3 (STAT3), a member of the Janus kinase (JAK)/STAT signaling pathway, is a central transcription factor that is activated by phosphorylation of a conserved tyrosine residue (Tyr705) in response to extracellular cytokines and growth factors and is an attractive target for anticancer drug discovery[2]. InS3-54-A18 (STAT3 Inhibitor XX), analog of inS3-54, is a potential lead inhibitor of STAT3, which suppresses STAT3-dependent luciferase expression in dose- and time-dependent manners with IC50 of 8.8-12.6 μM[3]. Wound healing was reduced to 64% and 76% by 5 μM inS3-54-A1 and invasion was reduced to 35% and 13% by 10 μM inS3-54-A1 for A549 and MDA-MB-231 cells, respectively. The expression of STAT3 downstream target genes cyclin D1, survivin, matrix metalloproteinase-9 and vascular endothelial growth factor (VEGF) was decreased in both cell lines following inS3-54-A18 treatment[3]. Oral treatment of inS3-54-A18 (200 mg/kg) significantly reduced tumor growth in a mouse xenograft model of A549 cells compared with the vehicle control treatment, but had no significant effect on mouse body weight[3].
作用机制	InS3-54-A18 acts as STAT3 inhibitor via targeting the DNA-binding domain of STAT3.

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.68mL 0.54mL 0.27mL	13.38mL 2.68mL 1.34mL	26.75mL 5.35mL 2.68mL

参考文献

[1]US20150094353 [2]Darnell JE Jr, Kerr IM, Stark GR. Jak-STAT pathways and transcriptional activation in response to IFNs and other extracellular signaling proteins. Science. 1994 Jun 3;264(5164):1415-21. doi: 10.1126/science.8197455. PMID: 8197455. [3]Huang W, Dong Z, Chen Y, Wang F, Wang CJ, Peng H, He Y, Hangoc G, Pollok K, Sandusky G, Fu XY, Broxmeyer HE, Zhang ZY, Liu JY, Zhang JT. Small-molecule inhibitors targeting the DNA-binding domain of STAT3 suppress tumor growth, metastasis and STAT3 target gene expression in vivo. Oncogene. 2016 Feb 11;35(6):783-92. doi: 10.1038/onc.2015.215. Epub 2015 Jun 15. Erratum in: Oncogene. 2016 Feb 11;35(6):802. PMID: 26073084.