Pinometostat (EPZ5676)

製品コードS7062 バッチS706208

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₀H₄₂N₈O₃

分子量

562.71

CAS No.

1380288-87-8

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

100 mg/mL (177.71 mM)

Ethanol (warmed with 50ºC water bath)

25 mg/mL (44.42 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (8.89mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 30%PEG 300 2 5%Tween80 3 60% ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (8.89mM)	Taking the 1 mL working solution as an example, add 50 μL of 1000 mg/mL clarified DMSO stock solution to 300 μL PEG300, mix evenly to clarify; add 50 μL Tween-80 to the above system, mix evenly to clarify; Then continue to add 600 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with K_i of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.
in vitro	EPZ-5676 reduces H3K79 dimethylation with a cellular IC50 of 2.6 nM in MV4-11 cells. EPZ-5676 treatment results in concentration- and time-dependent reduction of H3K79 methylation without effect on the methylation status of other histone sites, which leads to inhibition of key MLL target genes and selective, apoptotic cell killing in MLL-rearranged leukemia cells. EPZ-5676 inhibits proliferation of MLL-AF4 rearranged cell line MV4-11 with an IC50 of 9 nM.
in vivo	EPZ-5676 continuously intravenous infusion for 21 days to xenograft model of MLL-rearranged leukemia, leads to dose-dependent anti-tumor activity. At the highest dose of 70.5 mg/kg/day, complete tumor regressions are achieved with no regrowth for up to 32 days after the cessation of treatment. No significant weight loss or obvious toxicity is observed in rats treated with EPZ-5676 during efficacy study.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MV4-11 cells
	濃度	0.003 uM
	反応時間	4 days
	実験の流れ	Cells were treated with various concentrations of EPZ-5676.
動物実験	動物モデル	NCr nu/nu mouse
	投薬量	20 mg/kg
	投与方法	i.p.

参考

http://webcast.aacr.org/p/2013annual/182
https://ash.confex.com/ash/2012/webprogram/Paper48109.html
https://pubmed.ncbi.nlm.nih.gov/23801631/

カスタマーフィードバック

: Data from [Data independently produced by , , Haematologica, 2018, 103(7):1110-1123]

: Data from [Data independently produced by , , Theranostics, 2018, 8(16):4359-4371]

: Data from [Data independently produced by , , Cell Rep, 2014, 9(3): 1163-70 ]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The lncRNA ELDR suppresses tumorigenicity of AML by interfering with DNA replication and chromatin accessibility [ Blood Adv, 2025, bloodadvances.2024015427]	PubMed: 40921006
A Model of Traumatic Brain Injury Oligomerizes Tau in Cortical Organoids and Induces Clinically Relevant Pathologies that Synergize with MAPT Mutation [ J Neurotrauma, 2025, 10.1177/08977151251374286]	PubMed: 40900146
Generation of musculoskeletal cells from human urine epithelium-derived presomitic mesoderm cells [ Cell Biosci, 2024, 14(1):93]	PubMed: 39010176
Distinct Responses to Menin Inhibition and Synergy with DOT1L Inhibition in KMT2A-Rearranged Acute Lymphoblastic and Myeloid Leukemia [ Int J Mol Sci, 2024, 25(11)6020]	PubMed: 38892207
Reprogramming human urine cells into intestinal organoids with long-term expansion ability and barrier function [ Heliyon, 2024, 10(13):e33736]	PubMed: 39040281
Diverse clonal fates emerge upon drug treatment of homogeneous cancer cells [ Nature, 2023, 620(7974):651-659]	PubMed: 37468627
Modelling acquired resistance to DOT1L inhibition exhibits the adaptive potential of KMT2A-rearranged acute lymphoblastic leukemia [ Exp Hematol Oncol, 2023, 12(1):81]	PubMed: 37740239
DOT1L activity affects neural stem cell division mode and reduces differentiation and ASNS expression [ EMBO Rep, 2023, e56233.]	PubMed: 37382163
H4K20me1 plays a dual role in transcriptional regulation of regeneration and axis patterning in Hydra [ Life Sci Alliance, 2023, 6(5)e202201619]	PubMed: 36944423
Modelling acquired resistance to DOT1L inhibition exhibits the adaptive potential of KMT2A-rearranged acute lymphoblastic leukemia [ Exp Hematol Oncol, 2023, 12(1):81]	PubMed: 37740239

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。