Pinometostat (EPZ5676)
Catalog No.S7062
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.
Cited by 1 Publication
1 Customer Review
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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.
Purity & Quality Control
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. | |||||||||||||||||||||||||||||||||||||
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| Targets |
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| 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. |
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| Cell Data |
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| 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 |
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