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EED226 纯度: 98.82%
EED226 是一种多梳抑制复合物 2 (PRC2) 抑制剂,与胚胎外胚层发育 (EED) 上的 K27me3 口袋结合,在移植瘤小鼠模型中具有强的抗肿瘤活性。EED226 是一种有效的,口服可生物利用的,选择性 EED 抑制剂。当 H3K27me0 肽用作体外酶法测定的底物时,EED226 抑制 PRC2 的 IC50 为 23.4 nM。
EED226 Chemical Structure
CAS No. : 2083627-02-3
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥660 | In-stock | |
5 mg | ¥600 | In-stock | |
10 mg | ¥900 | In-stock | |
25 mg | ¥1500 | In-stock | |
50 mg | ¥2500 | In-stock | |
100 mg | ¥4500 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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EED226 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Epigenetics Compound Library
- Histone Modification Research Compound Library
- Anti-Cancer Compound Library
- Reprogramming Compound Library
- Orally Active Compound Library
- Chemical Probe Library
- Anti-Blood Cancer Compound Library
- Targeted Diversity Library
生物活性 |
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model[1]. EED226 is a potent, selective, and orally bioavailable EED inhibitor[2]. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays[3]. |
IC50 & Target |
IC50: 23.4 nM (PRC2)[3] |
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体外研究 (In Vitro) |
EED226 is a highly potent, efficient and selective inhibitor of EZH2 and EZH1 evaluated against a broad range of epigenetic and non-epigenetic targets. It potently reduces global H3K27Me3 mark in cells and demonstrates selectively cell killing effects in cells carrying a heterozygous Y641N mutation. EED226 has moderate permeability as the measured in Caco-2 cells at A→B=3.0×10-6 cm/s, with an efflux ratio at 7.6[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
EED226 induces robust and sustained tumor regression in EZH2MUT pre-clinical DLBCL model. In CD-1 mice, dosing of EED226 for 14 days at 300 mg/kg bid is well tolerated with no apparent adverse effects. It has very low in vivo clearance, and approximately 100% oral bioavailability. EED226 has low volume of distribution (0.8 L/kg), reasonable terminal t1/2 (2.2 h), and moderate plasma protein binding (PPB)[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
369.40 |
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Formula |
C17H15N5O3S |
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CAS 号 |
2083627-02-3 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 29 mg/mL (78.51 mM) * “≥” means soluble, but saturation unknown. 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Animal Administration [2] |
Mice: EED226 is formulated as a suspension in 0.5% PHMC+0.5% Tween 80 in water and administered orally by gavage at a dose volume of 10 mL/kg to the tumor bearing mice. At the end point, the animals is given the first dose administration. For PK analysis 100 μL of blood samples are collected from each animal by orbital sinus bleeding. For analysis of compound levels and PD in tissues, tumors are collected 4 hr post treatment and frozen immediately in liquid nitrogen. Tumor and body weight change data are analyzed statistically[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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参考文献 |
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