CPI-360CAS号： 1802175-06-9分子式： C25H31N3O4 分子量： 437.53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 | |
| 描述 |
CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
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| 纯度 |
99.72 %
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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 | |
| 可溶性/溶解性 |
体外:
DMSO 20mg/mLwarming(45.71mM) Ethanol 18mg/mLwarming(41.14mM) Water <1mg> 10%DMSO+60%PEG400+ddH2O 20mg/mL |
| 生物活性 | |
| 靶点 |
EZH1
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| In vitro(体外研究) |
In KARPAS-422 cells, CPI-360 potently reduces global H3K27me3 and H3K27me2 levels with EC50 of 56 nM and 65 nM, respectively. CPI-360 also causes time-dependent transcriptional changes, and affects the viability of Y641N mutant EZH2-containing KARPAS-422 cells. In addition, CPI-360 gradually arrests KARPAS-422 cells in the G1 cell cycle stage followed by the induction of apoptosis.
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| In vivo(体内研究) |
In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%.
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| 参考文献 | |
| 参考文献 |
[1] Bradley WD, et al. Chem Biol. 2014, 21(11), 1463-1475. |
分子结构图
