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EPZ004777 2017-05-19T11:28:30+00:00

This dataset summarizes current cancer research data on EPZ004777, a DOT1L (KMT4)-specific inhibitor1. EPZ004777 displays a near absolute specificity for DOT1L as compared to other lysine or arginine methyltransferases including CARM1, EHMT2, EZH1, EZH2, PRMT1, PRMT5, PRMT8, SETD7, and WHSC1. The dataset is meant to help you choose the optimal cell lines (e.g. EPZ004777-sensitive or resistant cell lines) as epigenetic model systems for the cancer under investigation. This page is periodically updated, so please check it again for new data that may be relevant to your research.

Most cell lines can be purchased from the American Type Culture Collection (ATCC) or from the Leibniz-Institut-German Collection of Microorganisms and Cell Cultures (Deutsche Sammlung von Mikroorganismen und Zellkulturen; DSMZ), and links to these repositories are provided whenever available.

Salient genetic characteristics such as chimeric fusion genes (e.g. MLL-AF4 fusion) or mutations (e.g. a mutation at the CDKN2A locus) are also listed.

This dataset is a work in progress and we rely on our members and readers to point us to data relevant to this dataset. We, therefore, welcome any information that you may provide that would help us make this dataset a useful tool for your research. You may email us at info@ces.b2sg.org.

To cite this dataset: S. Winkler & I.M. Bennani-Baiti. EPZ004777 experimental data, histone methyltransferase inhibitor dataset. Cancer Epigenetics Drug Database (CEDD) v0.1, Cancer Epigenetics Society (http://ces.b2sg.org/cedd/hmti-2/epz004777/), 2016.

References:

  1. Daigle SR, Olhava EJ, et al., Richon VM, Pollock RM. Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor. Cancer Cell 20: 53-65, 2011.
Cancer Cell Line
Genetic Background
P/M
Functional Assay IC50 (µM)*
Acute lymphoblastic leukemia RS4;11 MLL-AF4; p53mut Cell proliferation 6.5
Acute monocytic leukemia THP-1 MLL-AF9 fusion Cell proliferation 3.5
Acute myeloblastic leukemia Kasumi-1 Cell proliferation 33
Acute myeloid leukemia EOL-1 Cell proliferation 0.7
KOPM-88 MLL-PTD P Cell proliferation 0.04
MOLM-13 MLL-AF9 fusion Cell proliferation 0.25-0.75
MUTZ-11 Cell proliferation 0.6
Acute promyelocytic leukemia HL-60 E2A-HLF fusion Cell proliferation > 10
Acute T cell leukemia Jurkat Cell proliferation > 50
Biphenotypic B-myelomonocytic leukemia MV4-11 MLL-AF4 fusion Cell proliferation 0.2
B cell precursor leukemia 697 E2A-PBX1 fusion Cell proliferation 37
KOPN-8 MLL-ENL fusion Cell proliferation 0.7
REH TEL-AML1 fusion Cell proliferation 14
SEM MLL-AF4 fusion Cell proliferation 1.8
Histiocytic lymphoma U937 Cell proliferation > 50
MUTZ-11 Cell proliferation 0.6