Molecular Formula | C30H42N8O3 |
Molar Mass | 562.71 |
Density | 1.45±0.1 g/cm3(Predicted) |
Boling Point | 835.3±75.0 °C(Predicted) |
pKa | 12.34±0.10(Predicted) |
Storage Condition | -20℃ |
In vitro study | EPZ-5676 reduced H3K79 bismethylation in MV4-11 cells with an IC50 of 2.6 nM. EPZ-5676 concentration-and time-dependent reduction of H3K79 methylation, while having no effect on other histone sites, resulted in inhibition of the key target MLL gene and selective apoptotic cell killing in MLL rearranged leukemia cells. EPZ-5676 inhibited MLL-AF4 proliferation of the rearranged cell line MV4-11 with an IC50 of 9 nM. EPZ-5676 reduced H3K79 bismethylation in MV4-11 of cells with an IC50 of 2.6 nM. EPZ-5676 concentration-and time-dependent reduction of H3K79 methylation, while having no effect on other histone sites, resulted in inhibition of the key target MLL gene and selective apoptotic cell killing in MLL rearranged leukemia cells. EPZ-5676 inhibited MLL-AF4 proliferation of the rearranged cell line MV4-11 with an IC50 of 9 nM. |
In vivo study | In the MLL-rearranged leukemia xenograft model, EPZ-5676 continuous intravenous drip resulted in dose-dependent antitumor activity after 21 days. At the highest dose of 70.5 mg/kg/day, treatment was discontinued after complete tumor regression and no tumor regrowth for up to 32 days. No significant weight loss or apparent toxicity occurred in EPZ-5676 of the treated rats. In the MLL-rearranged leukemia xenograft model, EPZ-5676 continuous intravenous infusion resulted in dose-dependent antitumor activity after 21 days. At the highest dose of 70.5 mg/kg/day, treatment was discontinued after complete tumor regression and no tumor regrowth for up to 32 days. No significant weight loss or apparent toxicity occurred in EPZ-5676 of the treated rats. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.777 ml | 8.886 ml | 17.771 ml |
5 mM | 0.355 ml | 1.777 ml | 3.554 ml |
10 mM | 0.178 ml | 0.889 ml | 1.777 ml |
5 mM | 0.036 ml | 0.178 ml | 0.355 ml |