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

目录号: HY-13803 纯度: 99.93%: Data Sheet SDS COA 产品使用指南
FAQs
技术支持

Tazemetostat (EPZ-6438) 是一种有效，选择性，口服的 EZH2 抑制剂。Tazemetostat 抑制含有 PRC2 复合体的野生型 EZH2 的活性， K_i 值为 2.5 ± 0.5 nM。Tazemetostat 抑制 EZH2，在肽测定和核小体测定中 IC₅₀ 分别为 11 和 16 nM。Tazemetostat 抑制大鼠 EZH2，IC₅₀ 为 4 nM。Tazemetostat 还抑制 EZH1，IC₅₀ 为 392 nM。 Tazemetostat 特异性诱导 SMARCB1 缺失的 MRT 细胞凋亡和分化。

MCE 的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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Tazemetostat Chemical Structure

CAS No. : 1403254-99-8

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥567	In-stock
1 mg	￥220	In-stock
5 mg	￥450	In-stock
10 mg	￥680	In-stock
50 mg	￥1700	In-stock
100 mg	￥2550	In-stock
200 mg	￥3800	In-stock
500 mg	现货	询价
1 g	现货	询价
5 g		询价
10 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Tazemetostat:

Tazemetostat (Standard) In-stock

MCE 顾客使用本产品发表的 77 篇科研文献

: Tazemetostat purchased from MCE. Usage Cited in: J Clin Invest. 2018 Jan 2;128(1):483-499. [Abstract]; Immunoblotting for N1-ICD (n=3) in mouse podocytes exposed to 10 μM EPZ-6438 for 48 hours.

: Tazemetostat purchased from MCE. Usage Cited in: Nat Struct Mol Biol. 2018 Mar;25(3):225-232. [Abstract]; Western blots of extracts from E14 mESCs treated with 10 μM. EPZ6438 EZH2 inhibitor for 7 d and sampled at time points following inhibitor washout. Blots are probed with the indicated antibodies.

: Tazemetostat purchased from MCE. Usage Cited in: Toxins. 2017 May 16;9(5). pii: E162. [Abstract]; Cells are treated with LeTx in the presence or absence of GSK-J4 or EPZ-6438 for 48 h. H3K27me3 level is analyzed by Western blotting.

Tazemetostat 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

生物活性
纯度 & 产品资料
参考文献

生物活性

Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K_i value of 2.5 nM. Tazemetostat inhibits EZH2 with IC₅₀s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC₅₀ of 4 nM. Tazemetostat also inhibits EZH1 with an IC₅₀ of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells^[1].

IC₅₀ & Target^[1]

EZH2

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
4T1	IC₅₀	29.3 μM Compound: EPZ-6438	Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
A2780	IC₅₀	47 μM Compound: EPZ-6438	Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
A549	IC₅₀	15.83 μM Compound: EPZ-6438	Antiproliferative activity against human A549 cells by MTT assay Antiproliferative activity against human A549 cells by MTT assay	[PMID: 38580135]
A549	IC₅₀	> 100 μM Compound: EPZ-6438	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
ASPC1	IC₅₀	> 30 μM Compound: EPZ6438	Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay	[PMID: 35500243]
BT-549	IC₅₀	15.36 μM Compound: Taz	Synergistic cytotoxicity against human BT-549 cells incubated for 72 hrs in presence of Niraparib by MTT assay Synergistic cytotoxicity against human BT-549 cells incubated for 72 hrs in presence of Niraparib by MTT assay	[PMID: 38134746]
BT-549	IC₅₀	57.46 μM Compound: Taz	Cytotoxicity against human BT-549 cells incubated for 72 hrs by MTT assay Cytotoxicity against human BT-549 cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
BT-549	IC₅₀	58.2 μM Compound: EPZ-6438	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
BT-549	IC₅₀	> 10 μM Compound: EPZ-6438	Anti-proliferative activity against human BT-549 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human BT-549 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]
BT-549	IC₅₀	> 40 μM Compound: Tazemetostat	Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
Breast carcinoma cell	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human 3D Triple-negative breast cancer cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human 3D Triple-negative breast cancer cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
CWR22R	GI₅₀	51.94 μM Compound: EPZ; EPZ6438	Growth inhibition of human 22Rv1 cells incubated for 6 to 7 days by MTS assay Growth inhibition of human 22Rv1 cells incubated for 6 to 7 days by MTS assay	[PMID: 39196854]
CWR22R	GI₅₀	> 30 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human 22Rv1 cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay Synergistic growth inhibition of human 22Rv1 cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay	[PMID: 39196854]
CWR22R	GI₅₀	> 30 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human 22Rv1 cells incubated for 6 to 7 days in presence of TCP by MTS assay Synergistic growth inhibition of human 22Rv1 cells incubated for 6 to 7 days in presence of TCP by MTS assay	[PMID: 39196854]
DB	IC₅₀	> 3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human DB cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human DB cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
Daudi	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Daudi cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human Daudi cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
Daudi	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Daudi cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Daudi cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
ES-2	IC₅₀	79 μM Compound: EPZ-6438	Antiproliferative activity against human ES2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human ES2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
Farage	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Farage cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Farage cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
G-401	EC₅₀	0.2 μM Compound: 4; EPZ-6438; Tazemetostat	Inhibition of methyltransferase activity of EZH2 in human G401 cells assessed as H3K27 trimethylation after 4 hrs by ELISA Inhibition of methyltransferase activity of EZH2 in human G401 cells assessed as H3K27 trimethylation after 4 hrs by ELISA	[PMID: 26769278]
HCT-116	IC₅₀	> 20 μM Compound: 5; EPZ6438	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
HEY	IC₅₀	> 100 μM Compound: EPZ-6438	Antiproliferative activity against human HEY cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HEY cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
HK-2	IC₅₀	> 40 μM Compound: Tazemetostat	Antiproliferative activity against human HK-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HK-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
HL-60	IC₅₀	> 20 μM Compound: 5; EPZ6438	Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
HL-60	IC₅₀	> 40 μM Compound: Tazemetostat	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
HT	IC₅₀	> 3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human HT cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human HT cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
HeLa	IC₅₀	0.02 μM Compound: EPZ-6438	Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method	[PMID: 26189078]
HeLa	IC₅₀	27.69 μM Compound: EPZ-6438	Antiproliferative activity against human HeLa cells by MTT assay Antiproliferative activity against human HeLa cells by MTT assay	[PMID: 38580135]
K562	IC₅₀	59.2 μM Compound: 2; EPZ-6438	Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 35569264]
KARPAS-422	GI₅₀	0.09 μM Compound: 1; EPZ-6438	Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
KARPAS-422	GI₅₀	0.39 μM Compound: 1; EPZ-6438	Antiproliferative activity against human KARPAS-422 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human KARPAS-422 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
KARPAS-422	IC₅₀	0.012 μM Compound: 5; EPZ-6438	Antiproliferative activity against human KARPAS422 cells harboring monoallelic Y641N EZH2 mutation assessed as reduction in cell viability measured every 3 to 4 days up to 14 days by Beckman Coulter-based method Antiproliferative activity against human KARPAS422 cells harboring monoallelic Y641N EZH2 mutation assessed as reduction in cell viability measured every 3 to 4 days up to 14 days by Beckman Coulter-based method	[PMID: 28092155]
KARPAS-422	IC₅₀	0.294 μM Compound: 1; EPZ-6438	Antiproliferative activity against human KARPAS-422 cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human KARPAS-422 cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
KARPAS-422	IC₅₀	3.86 nM Compound: 1; EPZ-6438	Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant	[PMID: 37956762]
KARPAS-422	IC₅₀	35.01 nM Compound: 1; EPZ-6438	Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method	[PMID: 38640588]
KMS-11	IC₅₀	> 20 μM Compound: EPZ6438	Antiproliferative activity against human KMS-11 cells assessed as inhibition of cell growth incubated for 6 days by CCK-8 assay Antiproliferative activity against human KMS-11 cells assessed as inhibition of cell growth incubated for 6 days by CCK-8 assay	[PMID: 36642961]
L02	IC₅₀	> 40 μM Compound: Tazemetostat	Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
LNCaP	GI₅₀	12 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human LNCaP cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay Synergistic growth inhibition of human LNCaP cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay	[PMID: 39196854]
LNCaP	GI₅₀	13 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human LNCaP cells incubated for 6 to 7 days in presence of TCP by MTS assay Synergistic growth inhibition of human LNCaP cells incubated for 6 to 7 days in presence of TCP by MTS assay	[PMID: 39196854]
LNCaP	GI₅₀	19.5 μM Compound: EPZ; EPZ6438	Growth inhibition of human LNCaP cells incubated for 6 to 7 days by MTS assay Growth inhibition of human LNCaP cells incubated for 6 to 7 days by MTS assay	[PMID: 39196854]
MCF-10A	IC₅₀	> 40 μM Compound: Taz	Cytotoxicity against human MCF-10A cells incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-10A cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
MCF-10A	IC₅₀	> 40 μM Compound: Taz	Synergistic cytotoxicity against human MCF-10A cells incubated for 72 hrs in presence of Niraparib by MTT assay Synergistic cytotoxicity against human MCF-10A cells incubated for 72 hrs in presence of Niraparib by MTT assay	[PMID: 38134746]
MCF-10A	IC₅₀	> 40 μM Compound: Tazemetostat	Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MCF-10A	IC₅₀	> 50 μM Compound: Taz	Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 34455779]
MCF7	IC₅₀	> 100 μM Compound: EPZ-6438	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
MCF7	IC₅₀	> 40 μM Compound: Tazemetostat	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MCF7	IC₅₀	> 50 μM Compound: 6; EPZ-6438	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 35531606]
MCF7	IC₅₀	> 50 μM Compound: Taz	Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 34455779]
MDA-MB-231	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human MDA-MB-231 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-231 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
MDA-MB-231	IC₅₀	11.07 μM Compound: Taz	Synergistic cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs in presence of Niraparib by MTT assay Synergistic cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs in presence of Niraparib by MTT assay	[PMID: 38134746]
MDA-MB-231	IC₅₀	44.45 μM Compound: Taz	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 34455779]
MDA-MB-231	IC₅₀	52.72 μM Compound: Taz	Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
MDA-MB-231	IC₅₀	> 20 μM Compound: 5; EPZ6438	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
MDA-MB-231	IC₅₀	> 40 μM Compound: Tazemetostat	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MDA-MB-468	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human MDA-MB-468 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-468 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
MDA-MB-468	IC₅₀	46.67 μM Compound: 6; EPZ-6438	Antiproliferative activity against human MDA-MB-468 cells Antiproliferative activity against human MDA-MB-468 cells	[PMID: 35531606]
MDA-MB-468	IC₅₀	46.76 μM Compound: Taz	Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 34455779]
MDA-MB-468	IC₅₀	> 2.5 μM Compound: EPZ-6438	Anti-proliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]
MDA-MB-468	IC₅₀	> 40 μM Compound: Tazemetostat	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MV4-11	IC₅₀	22.38 μM Compound: EPZ-6438	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 31959420]
MV4-11	IC₅₀	> 20 μM Compound: 5; EPZ6438	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
MV4-11	IC₅₀	> 40 μM Compound: Tazemetostat	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
Medulloblastoma cell	IC₅₀	8.74 μM Compound: Chemical Probe: EPZ6438	Antiproliferative activity in Ptch1-deficient mouse medulloblastoma cell after 48 hrs by CCK-8 assay Antiproliferative activity in Ptch1-deficient mouse medulloblastoma cell after 48 hrs by CCK-8 assay	[PMID: 32579914]
NCI-H1703	IC₅₀	> 100 μM Compound: EPZ-6438	Antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
OAW-42	IC₅₀	> 100 μM Compound: EPZ-6438	Antiproliferative activity against human OAW-42 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human OAW-42 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
OPM-2	IC₅₀	> 3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human OPM-2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human OPM-2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
OVCAR-3	IC₅₀	> 100 μM Compound: EPZ-6438	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
PA-1	IC₅₀	46.6 μM Compound: EPZ-6438	Antiproliferative activity against human PA-1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human PA-1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
PC-3	GI₅₀	> 30 μM Compound: EPZ; EPZ6438	Growth inhibition of human PC-3 cells incubated for 6 to 7 days by MTS assay Growth inhibition of human PC-3 cells incubated for 6 to 7 days by MTS assay	[PMID: 39196854]
PC-3	GI₅₀	> 30 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human PC-3 cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay Synergistic growth inhibition of human PC-3 cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay	[PMID: 39196854]
PC-3	GI₅₀	> 30 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human PC-3 cells incubated for 6 to 7 days in presence of TCP by MTS assay Synergistic growth inhibition of human PC-3 cells incubated for 6 to 7 days in presence of TCP by MTS assay	[PMID: 39196854]
Pfeiffer	GI₅₀	0.002 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
Pfeiffer	GI₅₀	0.01 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Pfeiffer cells expressing A677G mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Pfeiffer cells expressing A677G mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
Pfeiffer	IC₅₀	0.034 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Pfeiffer cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human Pfeiffer cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
Pfeiffer	IC₅₀	2.26 nM Compound: 1; EPZ-6438	Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant	[PMID: 37956762]
Pfeiffer	IC₅₀	38 nM Compound: EPZ-6438	Cytotoxicity against human Pfeiffer cells assessed as decrease in cell viability after 5 days by CellTiter-Glo reagent based luminescence assay Cytotoxicity against human Pfeiffer cells assessed as decrease in cell viability after 5 days by CellTiter-Glo reagent based luminescence assay	[PMID: 29456795]
RD	CC₅₀	244.78 μM Compound: Tazemetostat	Cytotoxicity against human RD cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human RD cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37021456]
Raji	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Raji cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human Raji cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
Raji	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
SK-BR-3	IC₅₀	67.1 μM Compound: EPZ-6438	Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
SK-OV-3	IC₅₀	89.8 μM Compound: EPZ-6438	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
SU-DHL-2	IC₅₀	> 3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human SUDHL2 cells expressing EZH2 mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human SUDHL2 cells expressing EZH2 mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
SU-DHL-6	GI₅₀	1.05 μM Compound: 1; EPZ-6438	Antiproliferative activity against human SU-DHL-6 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human SU-DHL-6 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
SU-DHL-6	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human SU-DHL-6 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-6 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
SU-DHL-6	IC₅₀	21.95 μM Compound: EPZ-6438	Antiproliferative activity against human SU-DHL-6 cells Antiproliferative activity against human SU-DHL-6 cells	[PMID: 38056296]
SU-DHL10	IC₅₀	> 20 μM Compound: 5; EPZ6438	Antiproliferative activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
SUD4	GI₅₀	3.39 μM Compound: 1; EPZ-6438	Antiproliferative activity against human SU-DHL-4 cells harboring EZH2 Y641S mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human SU-DHL-4 cells harboring EZH2 Y641S mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
SUD4	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human SU-DHL-4 cells expressing Y641S mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-4 cells expressing Y641S mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
SUD4	IC₅₀	14.34 μM Compound: EPZ-6438	Antiproliferative activity against over expressing E2H2 human SUDHL4 cells Antiproliferative activity against over expressing E2H2 human SUDHL4 cells	[PMID: 31959420]
SW982	CC₅₀	116.43 μM Compound: Tazemetostat	Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37021456]
U2932	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human U2932 cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human U2932 cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
U2932	IC₅₀	> 3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human U2932 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human U2932 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
WSUDLCL2	GI₅₀	> 10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human WSUDLCL2 cells expressing Y641F mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human WSUDLCL2 cells expressing Y641F mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
WSUDLCL2	IC₅₀	6.44 nM Compound: 1; EPZ-6438	Antiproliferative activity against human WSUDLCL2 cells harboring EZH2 Y641F mutant Antiproliferative activity against human WSUDLCL2 cells harboring EZH2 Y641F mutant	[PMID: 37956762]
WSUDLCL2	IC₅₀	> 3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human WSUDLCL2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human WSUDLCL2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]

体外研究
(In Vitro)

Tazemetostat (EPZ-6438) 抑制多种野生型和突变型淋巴瘤细胞系增殖，IC₅₀ 为 0.49 nM-7.6 μM^[1]。

MCE 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
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 或 500 mg/kg，每天两次，持续 21-28 天) 几乎可以消除快速生长的 G401 肿瘤^[1]。

MCE 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.

Clinical Trial

分子量

572.74

Formula

C₃₄H₄₄N₄O₄

CAS 号

1403254-99-8

性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 58.33 mg/mL (101.84 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7460 mL	8.7300 mL	17.4599 mL
5 mM	0.3492 mL	1.7460 mL	3.4920 mL
10 mM	0.1746 mL	0.8730 mL	1.7460 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (4.36 mM); 澄清溶液
方案二

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.36 mM); 澄清溶液
方案三

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.63 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案四

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.63 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案五

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.63 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 0.5% CMC-Na/0.1% Tween-80 in Saline water
Solubility: 50 mg/mL (87.30 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.93%

选择批次：

Data Sheet (639 KB) SDS (393 KB)

COA (290 KB) HNMR (206 KB) LCMS (120 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

Tazemetostat 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7460 mL	8.7300 mL	17.4599 mL	43.6498 mL
	5 mM	0.3492 mL	1.7460 mL	3.4920 mL	8.7300 mL
	10 mM	0.1746 mL	0.8730 mL	1.7460 mL	4.3650 mL
	15 mM	0.1164 mL	0.5820 mL	1.1640 mL	2.9100 mL
	20 mM	0.0873 mL	0.4365 mL	0.8730 mL	2.1825 mL
	25 mM	0.0698 mL	0.3492 mL	0.6984 mL	1.7460 mL
	30 mM	0.0582 mL	0.2910 mL	0.5820 mL	1.4550 mL
	40 mM	0.0436 mL	0.2182 mL	0.4365 mL	1.0912 mL
	50 mM	0.0349 mL	0.1746 mL	0.3492 mL	0.8730 mL
	60 mM	0.0291 mL	0.1455 mL	0.2910 mL	0.7275 mL
	80 mM	0.0218 mL	0.1091 mL	0.2182 mL	0.5456 mL
	100 mM	0.0175 mL	0.0873 mL	0.1746 mL	0.4365 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tazemetostat1403254-99-8EPZ-6438 E-7438EPZ6438EPZ 6438E7438E 7438E-7438Histone MethyltransferaseApoptosisEZH2PRC2EZH1epigeneticcancerInhibitorinhibitorinhibit

产品名称：			* 需求量：
* 客户姓名：			* Email：
* 电话：			* 公司或机构名称：
留言给我们：

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2025 MedChemExpress. All Rights Reserved.

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

Customer Review

Other Forms of Tazemetostat:

MCE 顾客使用本产品发表的 77 篇科研文献

Tazemetostat 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Histone Methyltransferase 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Tazemetostat 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

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

Customer Review

Other Forms of Tazemetostat:

Tazemetostat 相关抗体

MCE 顾客使用本产品发表的 77 篇科研文献

Tazemetostat 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Histone Methyltransferase 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Tazemetostat 相关抗体:

摩尔计算器

稀释计算器

Tazemetostat 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z