PTC-209 HBrCAS号： 1217022-63-3分子式： C17H13Br2N5OS.HBr分子量： 576.10描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 |
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| 描述 |
PTC-209 HBr is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs).
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| 纯度 |
98%
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| 储存/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.
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| 基本信息 |
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| 可溶性/溶解性 |
DMSO:100 mg/mL warmed (173.58 mM)
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| 生物活性 |
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| 靶点 |
BMI-1
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| In vitro(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.
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| In vivo(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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| 参考文献 |
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| 参考文献 |
1. Kreso A, et al. Nat Med. 2014, 20(1), 29-36.
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