CPI-169CAS号： 1450655-76-1分子式： C27H36N4O5S分子量： 528.66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-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively. |
| 纯度 |
98%
|
| 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.
|
| 基本信息 | |
| 可溶性/溶解性 |
DMSO ：100mg/mL(189.15mM)
Ethanol ：100mg/mL(189.15mM) |
| 生物活性 | |
| 靶点 |
EZH2 WT,EZH2 Y641N,EZH1
|
| In vitro(体外研究) |
In KARPAS-422 cells, CPI-169 shows a dose-dependent inhibitory effect on cell viability, and produces synergy anti-proliferative activity when used in combination with ABT-199. In 16 out of 25 NHL cell lines, CPI-169 also suppresses cell growth with GI50 of
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| In vivo(体内研究) |
In mice bearing KARPAS-422 xenografts, CPI-169 (200 mg/kg, s.c.) effectively suppresses H3K27me3 levels and results in lymphoma tumor regression without affecting body weight or causing any overt adverse effects.
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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
