产品
编 号:F671345
分子式:C89H171F3N52O21S2
分子量:2426.77
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1mg
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5mg
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10mg
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生物活性:
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice.

体内研究:
GO-203 (18mg/kg/天;腹腔注射;持续 28 天) TFA 显着抑制 COLO-205 肿瘤的生长。Animal Model:Four- to 6-week-old BALB/c nu/nu male/female mice with Colo-205 or SKCO-1 cells
Dosage:18 mg/kg
Administration:IP; daily; for 28 days
Result:Significantly inhibited growth of the COLO-205 tumors. These tumors regressed completely by the end of treatment (day 28) and there was no evidence for regrowth by day 180.

体外研究:
GO-203 TFA (5 μM;三天) 通过降低细胞内 GSH 水平和增强 ROS 产生来抑制 MUC1 阳性结直肠癌细胞增殖。GO-203 TFA 对 MUC1 阴性 SW480 和 LOVO 细胞的细胞生长没有影响。GO-203 (5 μM;三天) TFA 诱导 SKCO-1 细胞约 80% 死亡。GO-203 TFA 导致线粒体膜电位显着降低。GO-203 (5 μM;持续三天) TFA 抑制结直肠癌细胞中的 AKT-mTORC-S6K1 翻译途径。GO-203 (5 μM;持续三天) TFA 显着降低 SKCO-1 细胞中的 GSH 水平。
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