Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 5-bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-ß-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Purity: ≥98%
Formula Markup: C28H40BrN7O4
Formula Weight: 618.6
CAS Number: 1561178-17-3
Notes: SGC0946 is an inhibitor of the non-SET domain-containing methyltransferase DOT1L (IC50 = 0.3 nM).{27033} It is selective for DOT1L over a panel of 12 additional protein methyltransferases, DNA methyltransferase 1 (DNMT1), and a panel of 29 receptors and ion channels. SGC0946 reduces the levels of dimethylated lysine 79 on histone 3 (H3K79me2) in MCF-10A breast cancer cells (IC50 = 8.8 nM). It selectively reduces the viability of isolated human cord blood cells transformed with an MLL-AF9 fusion oncogene over those transformed with a TLS-ERG fusion oncogene when used at concentrations of 1 and 5 µM. Adoptive transfer of isolated human CD3+ T cells pre-incubated with SGC0946 (0.5 µM) prevents weight loss, increases survival, and reduces hepatic and colonic lymphocyte infiltration in a xenogeneic mouse model of graft versus host disease (GVHD).{69946}
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