Tazemetostat hydrochloride(Synonyms: 他泽司他盐酸盐; EPZ-6438 hydrochloride; E-7438 hydrochloride)

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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 hydrochloride (Synonyms: 他泽司他盐酸盐; EPZ-6438 hydrochloride; E-7438 hydrochloride)

Tazemetostat (EPZ-6438) hydrochloride 是一种有效、选择性和口服活性的 EZH2 抑制剂，EZH2 肽和 EZH2 核小体的 IC50 值分别为 11 和 16 nM。Tazemetostat hydrochloride 可用于癌症研究。

Tazemetostat hydrochloride(Synonyms: 他泽司他盐酸盐; EPZ-6438 hydrochloride; E-7438 hydrochloride)

Tazemetostat hydrochloride Chemical Structure

CAS No. : 1467052-84-1

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Tazemetostat hydrochloride 的其他形式现货产品:

Tazemetostat Tazemetostat hydrobromide

生物活性

Tazemetostat (EPZ-6438) hydrochloride is a potent, selective and orally active EZH2 inhibitor with IC50 values of 11 and 16 nM for EZH2 peptide and nucleosome, respectively. Tazemetostat hydrochloride can be used for cancer research[1].

体外研究
(In Vitro)

Tazemetostat (EPZ-6438; 0.49-7.6 μM, 11 days) hydrochloride inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49-7.6 μM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: Wild-type and mutant lymphoma cell lines
Concentration: 0.49-7.6 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; 250-500 mg/kg; p.o.; twice daily; for 21-28 days) hydrochloride practically eliminates the fast-growing G401 tumors[1].

Shanghai Jinpan Biotech Co Ltd 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 and 500 mg/kg
Administration: Oral administration; twice daily; 28 days
Result: Eliminated the fast-growing G401 tumors.

分子量

609.20

Formula

C34H45ClN4O4
CAS 号

1467052-84-1
中文名称

他泽司他盐酸盐
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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