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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-CPI-360
CPI-360

Chemical Structure : CPI-360

CAS No.: 1802175-06-9

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CPI-360 (CPI 360)

货号: PC-21930Not For Human Use, Lab Use Only.

CPI-360 is a potent, selective EZH2 inhibitor with IC50 of 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively.

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5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CPI-360 is a potent, selective EZH2 inhibitor with IC50 of 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively.
CPI-360 decreases cellular levels of H3K27me3 and H3K27me2 (EC50, 56 and 65 nM, respectively), triggering cell cycle arrest and ultimately resulting in apoptosis in a large panel of non-Hodgkin's lymphoma (NHL) cell lines.
CPI-360 (200 mg/kg) reduced tumor growth of KARPAS-422 xenografts in mice.

物理化学性质&存储条件

分子量 437.54
分子式 C25H31N3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-[(1,2-Dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]-1H-indole-3-carboxamide

参考文献

1. Gehling VS, et al. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3644-9.

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