Tazemetostat trihydrochloride(Synonyms: EPZ-6438 trihydrochloride; E-7438 trihydrochloride)

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。

Tazemetostat trihydrochloride (Synonyms: EPZ-6438 trihydrochloride; E-7438 trihydrochloride)

Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) 是一种有效,选择性,口服的 EZH2 抑制剂。Tazemetostat trihydrochloride 抑制含有 PRC2 复合体的野生型 EZH2 的活性, Ki 值为 2.5 nM。Tazemetostat trihydrochloride 抑制 EZH2,在肽测定和核小体测定中 IC50 分别为 11 和 16 nM。Tazemetostat trihydrochloride 抑制大鼠 EZH2,IC50 为 4 nM。Tazemetostat trihydrochloride 还抑制 EZH1,IC50 为 392 nM。

Tazemetostat trihydrochloride(Synonyms: EPZ-6438 trihydrochloride; E-7438 trihydrochloride)

Tazemetostat trihydrochloride Chemical Structure

CAS No. : 1403255-00-4

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

* Please select Quantity before adding items.

Tazemetostat trihydrochloride 的其他形式现货产品:

Tazemetostat Tazemetostat hydrobromide

生物活性

Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM[1].

IC50 & Target[1]

EZH2 WT

2.5 nM (Ki)

EZH2

11 nM (IC50, in peptide assay)

EZH2

16 nM (IC50, in nucleosome assay)

Rat EZH2

4 nM (IC50)

EZH1

392 nM (IC50)

体外研究
(In Vitro)

Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM[1].

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.

Cell Proliferation Assay[1]

Cell Line: Wild-type and mutant lymphoma cell lines: DOHH-2 cell (EZH2 wild-type), Farage cell (EZH2 wild-type), OCI-LY19 cell (EZH2 wild-type), Toledo cell (EZH2 wild-type), KARPAS-422 (EZH2 Y646N), Pfeiffer (EZH2 A682G), RL cell line (EZH2 Y646N), SU-DHL-10 (EZH2 Y646F), SU-DHL-6 (EZH2 Y646N), WSU-DLCL2 (EZH2 Y646F)
Concentration: 0.49 nM-7.6 μM
Incubation Time: 11 days
Result: Inhibited DOHH-2 cell (EZH2 wild-type; IC50=1.7 μM), Farage cell (EZH2 wild-type; IC50=99 nM), OCI-LY19 cell (EZH2 wild-type; IC50=6.2 μM), Toledo cell (EZH2 wild-type; IC50=7.6 μM), KARPAS-422 (EZH2 Y646N; IC50=1.8 nM), Pfeiffer (EZH2 A682G; IC50=0.49 nM), RL cell line (EZH2 Y646N; IC50=5.8 μM), SU-DHL-10 (EZH2 Y646F; IC50=5.8 nM), SU-DHL-6 (EZH2 Y646N; IC50=4.7 nM), WSU-DLCL2 (EZH2 Y646F; IC50=8.6 nM) proliferation.

体内研究
(In Vivo)

Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors[1].

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.

Animal Model: SCID mice bearing s.c. G401 xenografts[1]
Dosage: 125 mg/kg, 250 mg/kg, 500 mg/kg
Administration: Oral; twice daily; 28 days
Result: Practically eliminated the fast-growing G401 tumors at 250 or 500 mg/kg.

Clinical Trial

分子量

682.12

Formula

C34H47Cl3N4O4

CAS 号

1403255-00-4

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]. Knutson SK, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferaseEZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7.

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