| Hazard Information | Back Directory | [Description]
HJC0416 is a potent orally bioavailable inhibitor of signal transducer and activator of transcription 3 (STAT3). | [Uses]
HJC0416 is a potent and orally active STAT3 inhibitor. HJC0416 shows antiprolifeative activity and induces apoptosis. HJC0416 decreases the expression of p-STAT3 (Tyr-705), Cyclin D1 and increases the expression of cleaved caspase-3 protein. HJC0416 shows anti-tumor activity[1]. | [in vivo]
HJC0416 (10 mg/kg for i.p.; 100 mg/kg for p.o.; daily for 7 days) reduces the tumor growth with no significant body weight loss in mice[1]. | Animal Model: | 6 weeks, female nude mice (MDA-MB-231 cells)[1] | | Dosage: | 10 mg/kg for i.p.; 100 mg/kg for p.o. | | Administration: | I.p. or p.o.; daily for 7 days | | Result: | Decreased the tumor volume for 67% as compared to the control mice for i.p.; the growth of xenograft tumors in mice was also significantly reduced at a dose of 100 mg/kg by 46%. |
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STAT3 | [References]
[1] Chen H, 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. DOI:10.1016/j.ejmech.2014.05.049 |
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