1. Epigenetics
  2. Histone Methyltransferase
  3. EEDi-5285

EEDi-5285 是一种非常有效且具有口服活性的胚胎外胚层发育 (EED) 抑制剂,结合 EED 蛋白的 IC50 值为 0.2 nM,并具有抗癌活性。

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EEDi-5285 Chemical Structure

EEDi-5285 Chemical Structure

CAS No. : 2488952-40-3

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规格 价格 是否有货 数量
1 mg ¥2320
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5 mg ¥5800
In-stock
10 mg ¥9800
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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity[1].

IC50 & Target

IC50: 0.2 nM (Embryonic ectoderm development (EED))[1]

体外研究
(In Vitro)

EEDi-5285 inhibits cell growth with IC50 values of 20 pM and 0.5 nM in the Pfeiffer and KARPAS422 lymphoma cell lines, respectively, carrying an EZH2 mutation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

EEDi-5285 (compound 28; 50-100 mg/kg; oral gavage; daily; for 28 days; SCID mice) treatment achieves complete and durable tumor regression in the KARPAS422 xenograft model in mice with oral administration[1].
A single 100 mg/kg oral administration of EEDi-5285 (compound 28) effectively reduces the level of H3K27me3 at 24 h in KARPAS422 tumor tissue in mice[1].
EEDi-5285 (compound 28) achieves a Cmax of 1.8 μM and an AUC of 6.0 h▪μg/ml with 10 mg/kg oral administration and has an oral bioavailability (F) of 75%. EEDi-5285 has a moderate volume of distribution of 1.4 L/kg and a terminal T1/2 of approximately 2 h[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice injected with KARPAS422 cells[1]
Dosage: 50 mg/kg, 100 mg/kg
Administration: Oral gavage; daily; for 28 days
Result: Showed highly efficacious and capable of achieving complete and long-lasting tumor regression in the KARPAS422 xenograft model in mice with oral administration.
分子量

479.53

Formula

C24H22FN5O3S

CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (260.67 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0854 mL 10.4269 mL 20.8538 mL
5 mM 0.4171 mL 2.0854 mL 4.1708 mL
查看完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.98%

参考文献

EEDi-5285 相关分类

完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0854 mL 10.4269 mL 20.8538 mL 52.1344 mL
5 mM 0.4171 mL 2.0854 mL 4.1708 mL 10.4269 mL
10 mM 0.2085 mL 1.0427 mL 2.0854 mL 5.2134 mL
15 mM 0.1390 mL 0.6951 mL 1.3903 mL 3.4756 mL
20 mM 0.1043 mL 0.5213 mL 1.0427 mL 2.6067 mL
25 mM 0.0834 mL 0.4171 mL 0.8342 mL 2.0854 mL
30 mM 0.0695 mL 0.3476 mL 0.6951 mL 1.7378 mL
40 mM 0.0521 mL 0.2607 mL 0.5213 mL 1.3034 mL
50 mM 0.0417 mL 0.2085 mL 0.4171 mL 1.0427 mL
60 mM 0.0348 mL 0.1738 mL 0.3476 mL 0.8689 mL
80 mM 0.0261 mL 0.1303 mL 0.2607 mL 0.6517 mL
100 mM 0.0209 mL 0.1043 mL 0.2085 mL 0.5213 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
EEDi-5285
目录号:
HY-136977
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