SC-1 是一种 SoRafenib 的衍生物,可抑制STAT3磷酸化,通过依赖 SHP-1 的STAT3失活诱导细胞凋亡,具有抗癌作用。
产品描述
SC-1 is a a derivative of the multiple tyrosine kinase inhibitor sorafenib. SC-1 potently inhibits the phosphorylation of STAT3 by blocking STAT3 phosphorylation and activation, and induces apoptosis in hepatocellular carcinoma cell lines[1].
体外活性
SC-1(1-10 μM; 48 hours; breast cancer cells) treatment demonstrates dose-dependent suppression of cell viability in all tested breast cancer cells[1]. SC-1(1-10 μM; 36 hours; breast cancer cells) treatment induces potent apoptotic activity in association with downregulation of p-STAT3 and its downstream proteins cyclin D1 and survivin in a dose-dependent manner in breast cancer cell lines[1].
体内活性
SC-1 showes efficacious antitumor activity and p-STAT3 downregulation in MDA-MB-468 xenograft tumors in vivo[1].
细胞实验
Incubated HCC-1937, MDA-MB-231, MDA-MB-468, MDA-MB-453, SK-BR3 and MCF-7 cells with 1 μM, 2 μM, 5 μM, 7.5 μM, 10 μM SC-1 for 48 hours demonstrated that dose-dependent suppression of cell viability in all tested breast cancer cells[1]. Incubated HCC-1937, MDA-MB-231, MDA-MB-468, MDA-MB-453, SK-BR3 and MCF-7 cells with 1 μM, 2 μM, 5 μM, 7.5 μM, 10 μM SC-1 for 36 hours showed downregulation of p-STAT3 and its downstream proteins cyclin D1 and survivin in a dose-dependent manner in breast cancer cell lines and induced potent apoptotic activity[1].
动物实验
SC-1 (10 mg/kg; oral gavage; daily; for 28 days; Female NCr athymic nude mice (4-6 weeks of age) injected with breast cancer cells) treatment shows efficacious antitumor activity and p-STAT3 downregulation in MDA-MB-468 xenograft tumors[1].
Cas No.
1313019-65-6
分子式
C21H13ClF3N3O2
分子量
431.8
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years