EPZ004777 formate
EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC50 being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 formate can be used for the study of leukemia.
For research use only. We do not sell to patients.
- Formula: C29H43N7O6
- Molecular Weight:585.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
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DOT1L 0.4 nM () |
Chemical Information
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Molecular Weight 585.70
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Formula C29H43N7O6
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SMILES
O=CO.NC1=NC=NC2=C1C=CN2[C@H]3[C@H](O)[C@H](O)[C@@H](CN(C(C)C)CCCNC(NC(C=C4)=CC=C4C(C)(C)C)=O)O3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Daigle SR, et al. Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor. Cancer Cell. 2011 Jul 12;20(1):53-65. [Content Brief]
[2]. Chen L, et al. Abrogation of MLL-AF10 and CALM-AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l. Leukemia. 2013 Apr;27(4):813-22. [Content Brief]
[3]. Deshpande AJ, et al. Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l.Blood. 2013 Mar 28;121(13):2533-41. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)