EEDi-5285

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

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。

EEDi-5285

EEDi-5285 Chemical Structure

CAS No. : 2488952-40-3

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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].

Shanghai Jinpan Biotech Co Ltd 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].

Shanghai Jinpan Biotech Co Ltd 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

2488952-40-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Rohan Kalyan Rej, et al. EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development. J Med Chem. 2020 Jul 9;63(13):7252-7267.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

发表回复