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Pinometostat

Pinometostat

产品编号 T3099   CAS 1380288-87-8
别名: EPZ-5676

Pinometostat (EPZ-5676) 是有效的DOT1L 组蛋白甲基转移酶抑制剂,Ki 为 80 pM。它可用于研究多种白血病治疗的实验。

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Pinometostat Chemical Structure
Pinometostat, CAS 1380288-87-8
规格 价格/CNY 货期 数量
1 mg ¥ 438 现货
2 mg ¥ 635 现货
5 mg ¥ 1,080 现货
10 mg ¥ 1,650 现货
25 mg ¥ 3,160 现货
50 mg ¥ 4,680 现货
100 mg ¥ 6,680 现货
1 mL * 10 mM (in DMSO) ¥ 1,360 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: Pinometostat (T3099)
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选择批次  
纯度: 99.83%
纯度: 99.29%
纯度: 99.19%
纯度: 97.56%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Pinometostat (EPZ-5676) has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leukemia, among others.
靶点活性 DOT1L:80 pM(Ki)
体外活性 EPZ-5676在最高剂量70.5 mg/kg/天时,使肿瘤完全消退,停止治疗后长达32天不再生长.用EPZ-5676治疗的大鼠没有观察到显著的体重减轻或明显的毒性.连续21天静脉内输注EPZ-5676至MLL重排白血病的异种移植模型,显示抗肿瘤活性,具有剂量依赖性.
体内活性 EPZ-5676处理导致H3K79甲基化的浓度和时间依赖性减少而不影响其他组蛋白位点的甲基化状态,这导致MLL重排白血病细胞中关键MLL靶基因和选择性凋亡细胞杀伤的抑制。在MV4-11细胞中EPZ-5676减少H3K79二甲基化,细胞IC50为2.6 nM。EPZ-5676抑制MLL-AF4重排细胞系MV4-11的增殖,IC50为9 nM。
细胞实验 EPZ-5676 is dissolved in DMSO. To analyse inhibition of histone methylation in MV4-11 cells following EPZ-5676 treatment, extracted histones (400 ng) are fractionated on a 10-20% Tris HCl gels with Tris-Glycine SDS running buffer under denaturing conditions and transferred to nitrocellulose filters. Filters are cut into strips and incubated for 1 hour in blocking buffer at room temperature (RT) and then incubated overnight at 4°C in blocking buffer. Filters are washed 3 times for 5 minutes with wash buffer (Phosphate buffered saline (PBS) including 0.01% Tween 20 (PBST)) and incubated with infrared tagged secondary antibody at RT for 1 hour. Filters are washed in PBST and reprobed for 1 hour at RT with the appropriate total histone antibody control (mouse anti-histone H3 (1:20,000), CST 3638, or mouse anti-histone H4 (1:10,000), CST 2935). Filters are washed again in PBST and incubated with infrared tagged secondary antibody (IRDye 800Cw donkey-anti-mouse IgG (1:20,000), Li-Cor 926-32212) at RT for 1 hour. After a final ish in PBST, filters are scanned using the Odyssey infared imager (Li-cor). To analyse inhibition of H3K79 methylation in peripheral blood mononuclear cells (PBMCs) from rats dosed with EPZ-5676, 20 μL of PBMC whole cell lysate is fractionated on denaturing gels and analysed by immunoblotting with antibodies to H3K79me2 or total H3. Signal intensities specific for the H3K79me2 antibody and total histone H3 control antibody are quantified using Odyssey software. The H3K79me2 signal intensity is normalized by dividing it by the total histone H3 control signal intensity in the same lane.
别名 EPZ-5676
分子量 562.71
分子式 C30H42N8O3
CAS No. 1380288-87-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 85 mg/mL (151.1 mM)

DMSO: 93 mg/mL (165.3 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.7771 mL 8.8856 mL 17.7711 mL 44.4279 mL
5 mM 0.3554 mL 1.7771 mL 3.5542 mL 8.8856 mL
10 mM 0.1777 mL 0.8886 mL 1.7771 mL 4.4428 mL
20 mM 0.0889 mL 0.4443 mL 0.8886 mL 2.2214 mL
50 mM 0.0355 mL 0.1777 mL 0.3554 mL 0.8886 mL
100 mM 0.0178 mL 0.0889 mL 0.1777 mL 0.4443 mL

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TargetMol Library Books参考文献

1. Robert A. Protein methyltransferases in cancer. AACR Annual Meeting, 2013. 2. Pollock RM, 54th ASH Annual Meeting and Exposition, 2012, Abst 2379 3. Chen R, Xie W, Cai B, et al. Establishment and Identification of a CiPSC Lineage Reprogrammed from FSP-tdTomato Mouse Embryonic Fibroblasts (MEFs)[J]. Stem cells international. 2018 Dec 25;2018:5965727.

TargetMol Library Books文献引用

1. Yu S, Zhou C, He J, et al. BMP4 drives primed to naïve transition through PGC-like state. Nature Communications. 2022, 13(1): 1-15 2. Chen R, Xie W, Cai B, et al. Establishment and Identification of a CiPSC Lineage Reprogrammed from FSP-tdTomato Mouse Embryonic Fibroblasts (MEFs). Stem Cells International. 2018 Dec 25;2018:5965727 3. Zhao X, Li X, Sun H, et al.Dot1l cooperates with Npm1 to repress endogenous retrovirus MERVL in embryonic stem cells.Nucleic Acids Research.2023: gkad640.
Sinefungin BAY-598 SW2_110A Amodiaquine dihydrochloride dihydrate CPUY074020 MS0124 PRMT5-IN-1 EZM0414

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 表观遗传库 临床期小分子药物库 抗COVID-19化合物库 经典已知活性库 抗癌临床化合物库 抑制剂库 药物功能重定位化合物库 高选择性抑制剂库 抗癌活性化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Pinometostat 1380288-87-8 Chromatin/Epigenetic Histone Methyltransferase EPZ5676 Inhibitor EPZ-5676 inhibit EPZ 5676 inhibitor

 

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