化合物EPZ004777 HCl,EPZ004777 hydrochloride

化合物 EPZ004777 HCl|T3081L|TargetMol

价格	询价
包装	1removed

最小起订量	1removed
发货地	上海
更新日期	2026-04-02

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产品详情

中文名称:化合物EPZ004777 HCl	英文名称:EPZ004777 hydrochloride
CAS:1380316-03-9	品牌: TargetMol
产地: 美国	保存条件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
纯度规格: 98%	产品类别: 抑制剂
货号: T3081L

Product Introduction

Bioactivity

名称	EPZ004777 hydrochloride
描述	EPZ004777 hydrochloride (EPZ004777 HCl) is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
细胞实验	EPZ004777 is prepared in DMSO (50 or 10 mM) and stored (?20°C), and then diluted with appropriate medium (DMSO 0.2%) before use[1]. For assessment of cell proliferation and viability in human cell lines, exponentially growing cells are plated, in triplicate, in 96-well plates at a density of 3×104 cells/well in a final volume of 150 μL. Cells are incubated in the presence of 3 μM (proliferation curve), or increasing concentrations (IC50 determination) of EPZ004777 up to 50 μM. Viable cell number is determined every 3-4 days for up to 18 days using the Guava Viacount assay and analyzed on a Guava EasyCyte Plus instrument. On days of cell counts, growth media and EPZ004777 are replaced and cells split back to a density of 5×104 cells/well. Total cell number is expressed as split-adjusted viable cells per well. For each cell line, IC50 values are determined from concentration-dependence curves at each time point using Graphpad Prism software. Experiments to determine IC50 values continued until IC50 values stabilized (day 18 for THP-1 cells, day 14 for all other cell lines)[1].
激酶实验	Avian (chicken) erythrocyte oligonucleosomes are purified. EPZ004777 is serially diluted 3-fold in DMSO for a total of ten concentrations, beginning at 1 μM. A 1 μL aliquot of each inhibitor dilution is plated in a 384-well microtiter plate. The 100% inhibition control consisted of 2.5 μM final concentration of the product inhibitor S-adenosyl-L-homocysteine, (SAH). Compound is incubated for 30 min with 40 μL per well of 0.25 nM DOT1L(1-416) in assay buffer (20 mM TRIS [pH 8.0] 10 mM NaCl, 0.002% Tween 20, 0.005% Bovine Skin Gelatin, 100 mM KCl, and 0.5 mM DTT). 10 μL per well of substrate mix comprising assay buffer with 200 nM 3H-SAM (80 Ci/mmol), 600 nM unlabeled SAM, and 20 nM nucleosomes are added to initiate the reaction (both substrates are present in the final reaction mixture at their respective KM values, an assay format referred to as "balanced conditions". Reactions are incubated for 120 min and quenched with 10 μL per well of 800 μM SAM. Incorporation of radioactivity into nucleosome substrate is measured in a flashplate. IC50 values for enzymes in the histone methyltransferase panel are determined under similar balanced assay conditions with both SAM and protein/peptide substrate present at concentrations equal to their respective KM values[1].
体外活性	EPZ004777 demonstrates potent, concentration-dependent inhibition of DOT1L enzyme activity with an IC50 of 400±100 pM. EPZ004777 displays remarkable selectivity for inhibition of DOT1L over other HMTs(PRMT5, 521±137 nM; others, >50 μM). The effect of extended EPZ004777 treatment is significantly specific for the MLL-rearranged cell lines. The number of viable MV4-11 and MOLM-13 cells is dramatically reduced by EPZ004777, whereas the growth of Jurkat cells is unaffected. A small population of MV4-11 cells remains viable in the presence of EPZ004777 while their number remains constant when growth curves are tracked over longer periods indicating that they have ceased to divide. The proliferation of MLL-AF9-transformed cells is strongly inhibited by EPZ004777 at concentrations of 3 μM or greater[1]. EPZ004777 selectively inhibits proliferation of MLL-AF10 and CALM-AF10 transformed murine bone marrow cells[2].
体内活性	EPZ004777 is well tolerated without overt toxicity observed. Complete blood count analysis after 14 days of continuous exposure to EPZ004777 revealed a statistically significant increase in the total white blood cell count, which resulted from an increase in neutrophils, monocytes, and lymphocytes. EPZ004777 (50, 100, or 150 mg/mL) administration is well tolerated, and no significant weight loss is observed[1].
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
溶解度	DMSO : Soluble
关键字	Inhibitor \| inhibit \| HistoneMethyltransferase \| Histone Methyltransferase \| EPZ-004777 Hydrochloride \| EPZ004777 hydrochloride \| EPZ-004777 \| EPZ004777 \| EPZ 004777 Hydrochloride \| EPZ 004777 \| DOT1L \| Apoptosis
相关产品	Formamide \| Urea \| Sodium Molybdate \| Dimethyl phthalate \| Aceglutamide \| Alginic acid \| Cysteamine hydrochloride \| Metronidazole \| Sildenafil citrate \| Citric Acid Triammonium \| Stavudine \| Tamoxifen

关键字： Inhibitor|||Apoptosis|||EPZ004777|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	2013-04-18 （14年）	注册资本	566.265100万人民币
员工人数	100-500人	年营业额	￥ 1亿以上
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务	经营模式	贸易,工厂,试剂,定制,服务

TargetMol中国（陶术生物）

VIP 4年

公司成立：14年
注册资本：566.265100万人民币
企业类型：有限责任公司(自然人投资或控股)
主营产品：小分子抑制剂、药物筛选化合物库、药物筛选等
公司地址：静安区江场三路238号8楼

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化合物 EPZ004777 HCl|T3081L|TargetMol相关厂家报价

产品名称	价格		公司名称	报价日期
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