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EEDi-5285
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EEDi-5285图片
CAS NO:2488952-40-3
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
EEDI5285
UM-EEDi-5285
产品介绍
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。

产品描述

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.

体外活性

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].

体内活性

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. 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. 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].

Cas No.

2488952-40-3

分子式

C24H22FN5O3S

分子量

479.53

别名

EEDI5285;UM-EEDi-5285

储存和溶解度

DMSO:112.5mg/mL (234.6mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years