货号	规格	价格	上海	北京	珠海	重庆	武汉
V47017-5mg	≥98%	￥1290.00 V47017-5mg ￥1290.00 3-5天	0 货期：3-5天	-	-	-	-
V47017-10mg	≥98%	￥2090.00 V47017-10mg ￥2090.00 3-5天	0 货期：3-5天	-	-	-	-
V47017-25mg	≥98%	￥4490.00 V47017-25mg ￥4490.00 3-5天	0 货期：3-5天	-	-	-	-
V47017-50mg	≥98%	￥7180.00 V47017-50mg ￥7180.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic . HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study.

靶点：

STAT3

体外研究：

HJC0416 hydrochloride (intraperitoneal injection; 10 mg/kg; 7 days) shows a 67% decrease of tumor volume as compared to the control mice. Similarly, HJC0416 hydrochloride (oral administration; 100 mg/kg; 14 days) also significantly reduces tumor volume at a dose of 100 mg/kg by 46%. The i.p. route appeared to have a better reduction of tumor volume. It is also noteworthy that HJC0416 does not show significant signs of toxicity at a dose of 100 mg/kg[1].

体内研究：

HJC0416 hydrochloride inhibits the proliferation of both ER-positive, and ER-negative (triple negative) breast cancer cells with IC50 values of 1.76 μM and 1.97 μM, respectively. However, it displays a marked antiproliferative effect against pancreatic cancer cell line AsPC1 and Panc-1 with IC50 values of 40 nM and 1.88 μM, respectively.
HJC0416 hydrochloride (1-10 μM; 48 hours) inhibits cell growth and induced apoptosis accompanying cellular morphological changes in MDA-MB-231 breast cancer cells.
HJC0416 hydrochloride (5 μM; 24 hours) decreases the STAT3 promoter activity by approximately 51%, while stattic only decreases the STAT3 promoter activity by 39% in MDA-MB-231 cells after transient transfecting with pSTAT3-Luc vector.
HJC0416 hydrochloride (1-10 μM; 12 hours) has a comparable potency in downregulating STAT3 protein production and phosphorylation at Tyr-705 site when compares with Stattic . Additionally, it also induces cleaved caspase-3 and downregulated cyclin D1 levels in MDA-MB-231 cells.

参考文献：

1. Haijun Chen, et al.Discovery of Potent Anticancer Agent HJC0416, an Orally Bioavailable Small Molecule Inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Eur J Med Chem. 2014 Jul 23;82:195-203.

保存条件：

-20°C, 避光,氮气保存

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.329 ml	11.647 ml	23.293 ml
5 mM	0.466 ml	2.329 ml	4.659 ml
10 mM	0.233 ml	1.165 ml	2.329 ml
50 mM	0.047 ml	0.233 ml	0.466 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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