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抑制剂描述:

产品名称:PTC-209

产品别名:见爱必信官网

英文别名:PTC-209

靶点:BMI-1;Autophagy

CAS:315704-66-6

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

PTC-209 is a specific inhibitor for BMI-1 with IC50 of 0.5 uM in in both GEMS reporter and ELISA assays.

溶解性:DMSO 99 mg/mL (199.92 mM)

体外研究:

PTC-209 inhibits both the UTR-mediated reporter expression and endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 decreases colorectal tumor cell growth in a BMI-1-dependent way. In addition, PTC-209 impairs colorectal cancer-initiating cells (CICs) through irreversible growth inhibition.

体内研究:PTC-209 (60 mg/kg/day, s.c.) effectively inhibits BMI-1 production in tumor tissue, and halts growth of preestablished tumors in mice bearing primary human colon cancer xenograft, human colon cancer cell lines LIM1215 or HCT116 xenografts. PTC-209 also reduces the frequency of functional colorectal CICs in vivo.

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