HJC0416 hydrochloride T40056

Product Introduction
Bioactivity


英文名: HJC0416 hydrochloride

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.

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

关键字: HJC-0416 Hydrochloride | HJC 0416 Hydrochloride | HJC-0416 hydrochloride | HJC0416 hydrochloride | HJC0416 Hydrochloride

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途