Pinometostat (EPZ5676)

目录号:S7062

Pinometostat (EPZ5676) Chemical Structure

Molecular Weight(MW): 562.71

Pinometostat (EPZ5676)是一种蛋白甲基转移酶DOT1L的S-腺苷甲硫氨酸(SAM)竞争性抑制剂,无细胞试验中Ki为80 pM,比作用于所有其他测试的PMTs选择性高37000倍以上,抑制肿瘤中H3K79甲基化。Phase 1。

规格 价格 库存 购买数量  
RMB 2218.64 现货
RMB 7924.04 现货
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客户使用该产品的4个实验数据:

  • Treatment of c-Kit+ bone marrow (BM) cells from Setd2f/f/Vav1-Cre mice with JQ1 500nM, EPZ-5676 1uM, BAY 1143572 400 nM for 24 h. Then cells were collected to determine the proteins levels of RNA pol II (Ser2P), pol II (Ser5P), Gata1, Gata3, Myc, and β-actin by immunoblotting.

    Haematologica, 2018, 103(7):1110-1123. Pinometostat (EPZ5676) purchased from Selleck.

    (A) HOXA9, PBX3, cleaved caspase 3 and cleaved PARP expression levels in OCI-AML2 and OCI-AML3 cells treated with EPZ5676 (10 µM) and harvested on the indicated day. Three independent western blotting replicates were performed.

    Theranostics, 2018, 8(16):4359-4371. Pinometostat (EPZ5676) purchased from Selleck.

  • Western blot validation of H3K79me2 depletion in Jurkat cells. Mixtures of 0%–100% EPZ5676-treated cells (0:100; 25:75; 50:50, 75:25; 100:0 proportions of [DMSO-treated:EPZ5676-treated] cells) were measured by immunoblot (IB) for the presence of H3K79me2, H3K4me3, or total histone H3 (loading control). Treated cells were exposed to 20 μM EPZ5676 for 4 days.

    Cell Rep, 2014, 9(3): 1163-70 . Pinometostat (EPZ5676) purchased from Selleck.

    Dot1l inhibitor decreases IL-6 and IFN-β production triggered by TLR ligands and virus infection. a, b Q-PCR a and ELISA b analysis of the mRNA and protein levels of IL-6 or IFN-β in mouse peritoneal macrophages treated with Dot1l inhibitor EPZ5676 (20 μM) or DMSO for 72 h and then stimulated with LPS (100 ng/ml) or Poly(I:C) (20 μg/ml) for 2 h a or 4 h b, or infected with VSV for 12 h a, b. c ChIP analysis of RNA polymerase II occupancy at the Il6 or Ifnb1 promoters in mouse peritoneal macrophages treated with Dot1l inhibitor EPZ5676 (20 μM) or DMSO for 72 h and then stimulated with LPS (100 ng/ml) or Poly(I:C) (20 μg/ml) for 2 h or infected with VSV (1 MOI) for 12 h. *P < 0.05; **P < 0.01; ***P < 0.001. Data are from three independent experiments (means ± s.e.m.)

    Cell Mol Immunol, 2018, doi: 10.1038/s41423-018-0170-4. Pinometostat (EPZ5676) purchased from Selleck.

产品安全说明书

Histone Methyltransferase抑制剂选择性比较

生物活性

产品描述 Pinometostat (EPZ5676)是一种蛋白甲基转移酶DOT1L的S-腺苷甲硫氨酸(SAM)竞争性抑制剂,无细胞试验中Ki为80 pM,比作用于所有其他测试的PMTs选择性高37000倍以上,抑制肿瘤中H3K79甲基化。Phase 1。
靶点
DOT1L [1]
(Cell-free assay)
80 pM(Ki)
体外研究

EPZ-5676减少了MV4-11细胞中H3K79双甲基化,IC50是2.6 nM。EPZ-5676浓度和时间依赖性降低H3K79甲基化,而对其他组蛋白位点无作用,这导致在MLL重排的白血病细胞中抑制的关键靶的MLL基因并选择性的凋亡细胞杀伤。EPZ-5676抑制MLL-AF4重新排列细胞系MV4-11的增殖,IC50为9 nM。

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MV4-11 cells NEHFOHZHfW6ldHnvckBie3OjeR?= MXK0JIRigXN? MWrJcohq[mm2aX;uJI9nKESRVEHMJIlvKGi3bXHuJG1XPC1zMTDj[YxteyCneIDy[ZN{cW6pIF3MUE1CTjRiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKEh|S{e5cYUzKGyndnXsJIFnfGW{IESg[IF6eyCkeTDFUGlUSSCvZYToc4Q> M{LhNlI2PDB4OEWz
human MOLM13 cells MX\Qdo9tcW[ncnH0bY9vKGG|c3H5 M1yyO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MUVE{KGOnbHzzJINwdnSjaX7pcochVUyOLVHGPUwhTUN3ME20JI5O MlO3NlM5Pzl2NkO=
human MV4-11 cells M4fPfnBzd2yrZnXyZZRqd25iYYPzZZk> NGPBV3BCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOE0yOSClZXzsd{Bkd262YXnubY5oKE2OTD3BSlQtKEWFNUC9OEBvVQ>? NHfuSm0zOzh5OUS2Ny=>
human THP1 cells MWrQdo9tcW[ncnH0bY9vKGG|c3H5 M{nWNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVFjQNUBk\WyuczDjc451[WmwaX7nJG1NVC2DRkmsJGVEPTB;NDDuUS=> MnrsNlM5Pzl2NkO=

... Click to View More Cell Line Experimental Data

体内研究 在MLL重排的白血病异种移植模型中,EPZ-5676连续静脉滴注21天后导致剂量依赖性的抗肿瘤活性。在最高剂量为70.5毫克/公斤/天时,肿瘤完全消退后治疗停止,长达32天都没有肿瘤再生长。在EPZ-5676治疗的大鼠中,无显著体重减轻或明显毒性出现。

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 100 mg/mL warmed (177.71 mM)
Ethanol 92 mg/mL warmed (163.49 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 562.71
化学式

C30H42N8O3

CAS号 1380288-87-8
稳定性 powder
in solvent
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03724084 Not yet recruiting Acute Myeloid Leukemia|KMT2A Gene Rearrangement National Cancer Institute (NCI) January 25 2019 Phase 1|Phase 2
NCT02141828 Completed Leukemia|Acute Myeloid Leukemia|Acute Lymphocytic Leukemia|Acute Leukemias Epizyme Inc.|Celgene Corporation May 2014 Phase 1
NCT01684150 Completed Acute Myeloid Leukemia|Acute Lymphoblastic Leukemia|Myelodysplastic Syndrome|Myeloproliferative Disorders Epizyme Inc.|Celgene September 2012 Phase 1

技术支持

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    Is the vehicle 30% PEG400/0.5% Tween80/5% propylene glycol recommended for in vivo use?

  • 回答:

    S7062 EPZ-5676 in 30% PEG400/0.5% Tween80/5% propylene glycol at 30 mg/ml is a suspension. For injection, 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml is suitable.

Histone Methyltransferase Signaling Pathway Map

Histone Methyltransferase Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID