化合物Fer and FerT inhibitor T4638

Product Introduction
Bioactivity


英文名: E260

描述: E260 (Fer and FerT inhibitor) 是Fer/FerT 激酶抑制剂。

体外活性: Fer and FerT inhibitor, which selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level. When applied to metastatic grade IV SW620 CC cells, which are serum starved for 16 h and treated with 3 mM H2O2 to activate Fer,Fer and FerT inhibitor exhibits inhibitory effects on the Fer-kinase activity as is reflected by suppressed auto-phosphorylation activity of the enzyme.

体内活性: Fer/FerT kinase inhibitor suppresses xenografts progression in vivo. The pharmacokinetic (PK) profile of Fer/FerT kinase inhibitor is determined in mice. Fer/FerT kinase inhibitor exhibits a T1/2?of 175 min in the blood, and a volume of distribution of 4244 mL/kg suggesting an efficient distribution of the compound in the animal tissues. To evaluate the efficacy of Fer/FerT kinase inhibitor on tumor growth, SW620 cells are subcutaneously introduced into immuno-compromised "Nude" mice. Administration of Fer/FerT kinase inhibitor leads to a significant attenuation of tumor progression throughout the experiment, and to a 10-fold decrease in average tumor volume after 22 days of treatment. To further demonstrate the anti-cancer activity of Fer/FerT kinase inhibitor in vivo, mice bearing SW48 cells derived xenografts are treated with Fer/FerT kinase inhibitor and the tumor progression profiles are determined. Mice treated with Fer/FerT kinase inhibitor demonstrate a 5-6-fold attenuation in tumors progression when compared to the control treated group

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

溶解度: DMSO : Slightly soluble


关键字: E 260 | Inhibitor | E260 | inhibit | E-260

相关库: Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library

化合物Fer and FerT inhibitor T4638信息由TargetMol中国为您提供，如您想了解更多关于化合物Fer and FerT inhibitor T4638报价、型号、参数等信息，欢迎来电或留言咨询。

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