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

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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

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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.

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