HJC0416 hydrochloride

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HJC0416 hydrochloride 

HJC0416 hydrochloride 是一种有效的口服活性 STAT3 抑制剂，具有比 Stattic (HY-13818) 更强的抗癌活性。HJC0416 hydrochloride 是一种很有前途的抗乳腺癌试剂。

HJC0416 hydrochloride

HJC0416 hydrochloride Chemical Structure

CAS No. : 2415263-08-8

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生物活性

HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study[1].

IC50 & Target[1]

STAT3

 

体外研究
(In Vitro)

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[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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

429.32

Formula

C18H18Cl2N2O4S
CAS 号

2415263-08-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vivo:
  • 1.

    All drugs were dissolved in 50% DMSO with 50% polyethylene glycol for in vivo administration[1].
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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