Molecular Formula | C46H47ClN8O9S
|
Molar Mass | 923.43 |
Density | 1.47±0.1 g/cm3(Predicted) |
Solubility | 10 mM in DMSO |
pKa | 10.74±0.40(Predicted) |
Storage Condition | 2-8°C(protect from light) |
In vitro study | In Burkitt's lymphoma cells, ARV-825 treatment resulted in more significant changes in c-MYC levels and downstream cell proliferation and apoptosis induction compared to other BRD4 inhibitors. Co-incubated with ARV-825 for 72 hours, ARV-825 had IC50 values in the 2-50 nM range against the cell lines tested and primary AML cells. In AML cells, ARV-825 reduces PIM1 levels and CXCR4 phosphorylation levels, and overexpression of PIM1 or CXCR4 reverses this effect. |
In vivo study | In the mouse model transplanted with human leukemia cells, the leukemia burden of the mice in the ARV-825 experimental group was significantly lower than that of the control group, and the survival time was longer than that of the control group. |