产品信息
抗原名称
EZH1
商品描述
CPI-360 is a potent, selective,and SAM-competitive <b>EZH1</b> inhibitor with <b>IC50</b> of 102.3 nM, >100-fold selectivity over other methyltransferases.
分子量
437.53
纯度
99.72 %
可溶性
体外:
DMSO 20mg/mLwarming(45.71mM)
Ethanol 18mg/mLwarming(41.14mM)
Water <1mg/mL
10%DMSO+60%PEG400+ddH2O 20mg/mL
DMSO 20mg/mLwarming(45.71mM)
Ethanol 18mg/mLwarming(41.14mM)
Water <1mg/mL
10%DMSO+60%PEG400+ddH2O 20mg/mL
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.
In vivo(体内研究)
In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%.
背景
分子式
C25H31N3O4
CAS号
1802175-06-9
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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