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HJC0416 hydrochloride

产品编号 T40056 CAS 2415263-08-8

HJC0416 hydrochloride, a potent, orally active inhibitor of STAT3, exhibits a superior anticancer profile compared to Stattic. It stands out as a promising agent for breast cancer research.

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HJC0416 hydrochloride Chemical Structure

HJC0416 hydrochloride, CAS 2415263-08-8

规格	价格/CNY		货期	数量
10 mg	￥ 3,810		35日内发货

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其他形式的 HJC0416 hydrochloride:

HJC0416
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参考文献

产品描述	HJC0416 hydrochloride, a potent, orally active inhibitor of STAT3, exhibits a superior anticancer profile compared to Stattic. It stands out as a promising agent for breast cancer research.
体外活性	HJC0416 hydrochloride inhibits the proliferation of both ER-positive, and ER-negative (triple negative) breast cancer cells with IC 50 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 IC 50 values of 40 nM and 1.88 μM, respectively[1].HJC0416 hydrochloride (1-10 μM; 48 hours) inhibits cell growth and induced apoptosis accompanying cellular morphological changes in MDA-MB-231 breast cancer cells[1].HJC0416 hydrochloride (5 μM; 24 hours) decreases the STAT3 promoter activity by approximately 51%, while stattic (HY-13818) only decreases the STAT3 promoter activity by 39% in MDA-MB-231 cells after transient transfecting with pSTAT3-Luc vector[1].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 (HY-13818). Additionally, it also induces cleaved caspase-3 and downregulated cyclin D1 levels in MDA-MB-231 cells[1]. Cell Cycle Analysis[1]Cell Line: MDA-MB-231 breast cancer cells Concentration: 1-10 μM Incubation Time: 48 hours Result: Induced cell apoptosis in cancer cells. Apoptosis Analysis[1]Cell Line: MDA-MB-231 breast cancer cells Concentration: 1 μM; 5 μM; 10 μM Incubation Time: 12 hours Result: Decreased p-STAT3 phosphorylation expression and cyclin D1 level.
体内活性	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]. Animal Model: Mice with MDA-MB-231 cells[1]Dosage: 10 mg/kg (i.p.); 100 mg/kg (oral) Administration: Intraperitoneal?injection, 7 days; oral administration, 14 days Result: Exhibited antitumor effects in the MDA-MB-231 triple-negative breast cancer murine xenograft model.

分子量	429.31
分子式	C18H18Cl2N2O4S
CAS No.	2415263-08-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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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.

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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