Pinometostat (EPZ5676)

Catalog No.S7062

Pinometostat (EPZ5676) Chemical Structure

Molecular Weight(MW): 562.71

Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki 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.

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1 Customer Review

  • 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.

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Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki 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.
Targets
DOT1L [1]
(Cell-free assay)
80 pM(Ki)
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.

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MV4-11 cells M4LkZ2Z2dmO2aX;uJIF{e2G7 NH;kNYI1KGSjeYO= NV\tSZJ3UW6qaXLpeIlwdiCxZjDEU3QyVCCrbjDoeY1idiCPVkStNVEh[2WubIOg[ZhxemW|c3nu[{BOVExvQV[0JIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDIN2s4QW2nMjDs[ZZmdCCjZoTldkA1KGSjeYOgZpkhTUyLU1GgcYV1cG:m MlnINlU1ODZ6NUO=
human MOLM13 cells M1u1SXBzd2yrZnXyZZRqd25iYYPzZZk> MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTF2xN{Bk\WyuczDjc451[WmwaX7nJG1NVC2DRkmsJGVEPTB;NDDuUS=> NGTNOFMzOzh5OUS2Ny=>
human MV4-11 cells NH;vNGZRem:uaX\ldoF1cW:wIHHzd4F6 MnXkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkStNVEh[2WubIOgZ49vfGGrbnnu[{BOVExvQV[0MEBGSzVyPUSgcm0> M2nGT|I{QDd7NE[z
human THP1 cells NXnk[JNsWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3K2NWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVFjQNUBk\WyuczDjc451[WmwaX7nJG1NVC2DRkmsJGVEPTB;NDDuUS=> NF7IemozOzh5OUS2Ny=>

... Click to View More Cell Line Experimental Data

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.

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (177.71 mM)
Ethanol 92 mg/mL warmed (163.49 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 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.

Chemical Information

Molecular Weight 562.71
Formula

C30H42N8O3

CAS No. 1380288-87-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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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