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Association details:
| Biomarker: | EZH2 Y641F |
|---|---|
| Cancer: | Melanoma |
| Drug: | JQEZ5 (EZH2 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
An oncogenic Ezh2 mutation cooperates with particular genetic alterations to induce tumors in mice and redistributes H3K27 trimethylation throughout the genome
Excerpt:
JQEZ5 was designed as an open-source compound with high potency and bioavailability, is ~10-fold selective for EZH2 over EZH1, and exhibits in vitro activity against the Y646F mutant in a homogenous assay (Supplementary Fig. 6a, b).
DOI:
10.1038/nm.4092
