PF-06726304 is a potent and selective EZH2 inhibitor with Ki value of 0.7 nM.
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产品名称 | Histone Methyltransferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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BRD4770 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
UNC1999 |
+++
EZH2, IC50: 2 nM EZH1, IC50: 45 nM |
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EPZ005687 |
++
EZH2, Ki: 24 nM |
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EPZ015666 |
+++
PRMT5, Ki: 5 nM |
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3-Deazaneplanocin A HCl |
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM |
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EPZ6438 |
+++
EZH2, IC50: 11 nM EZH2, Ki: 2.5 nM |
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GSK126 |
++
EZH2, IC50: 9.9 nM |
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MI-3 |
+
Menin-MLL, IC50: 648 nM |
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MM-102 |
++
MLL1, IC50: 0.4 μM |
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EI1 |
++
Ezh2 (wild-type), IC50: 15 nM EZH2 (Y641F), IC50: 13 nM |
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SGC0946 |
++++
DOT1L, IC50: 0.3 nM |
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PFI-2 HCl |
++++
SETD7, IC50: 2 nM SETD7, Ki: 0.33 nM |
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Pinometostat |
++++
DOT1L, Ki: 80 pM |
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EPZ004777 |
+++
DOT1L, IC50: 0.4 nM |
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Entacapone |
++
COMT, IC50: 151 nM |
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UNC0379 |
+
SETD8, IC50: 7.9 μM |
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Menin-MLL inhibitor MI-2 |
+
Menin-MLL, IC50: 446 nM |
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GSK343 |
+++
EZH2, IC50: 4 nM EZH1, IC50: 240 nM |
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BIX-01294 3HCl |
+
G9a, IC50: 2.7 μM |
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibited EZH2-WT and EZH2-Y641N mutant with Ki values of 0.7 and 3.0 nM, respectively. PF-06726304 inhibited H3K27me3 in Karpas-422 with an IC50 value of 15 nM. PF-06726304 has strong anti-tumour growth activity[1]. PF-06726304 inhibited the proliferation of Karpas-422 cells carrying wild-type EZH2 with an IC50 of 25 nM[1] . |
Animal study | In a subcutaneous Karpas-422 xenograft model, PF-06726304 inhibited tumour growth and induced potent modulation of downstream biomarkers at doses of 200 and 300 mg/kg, BID, administered for 20 days[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.24mL 0.45mL 0.22mL |
11.20mL 2.24mL 1.12mL |
22.41mL 4.48mL 2.24mL |
CAS号 | 1616287-82-1 |
分子式 | C22H21Cl2N3O3 |
分子量 | 446.326 |
别名 | PF-6726304 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 14 mg/mL(31.37 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |