Molecular Formula | C19H18ClN5OS |
Molar Mass | 399.9 |
Density | 1.51±0.1 g/cm3(Predicted) |
Boling Point | 690.4±65.0 °C(Predicted) |
Appearance | powder |
Color | white to beige |
pKa | 16.00±0.40(Predicted) |
Storage Condition | 2-8°C |
In vitro study | CPI203 inhibits BRD4 in vitro and in cells without affecting BRD4 kinase activity in vitro. CPI203 showed cell growth inhibition in all 9 MCL cell lines with GI50 ranging from 0.06 to 0.71 μm and low toxicity in normal PBMCs of healthy volunteers. In addition, lenalidomide and CPI203, targeting IRF4 and MYC, effectively activate the cell death program of bortezomib-resistant MCL cells. CPI203 inhibits BRD4 in vitro and in cells without affecting BRD4 kinase activity in vitro. CPI203 showed cell growth inhibition in all 9 MCL cell lines with GI50 ranging from 0.06 to 0.71 μm and low toxicity in normal PBMCs of healthy volunteers. In addition, lenalidomide and CPI203, targeting IRF4 and MYC, effectively activate the cell death program of bortezomib-resistant MCL cells. |
In vivo study | BRD4 regulates the phosphorylation of CTD Ser2 in vivo. In REC-1 tumor-bearing mice, lenalidomide combined with CPI203 (2.5 mg/kg, I. P.) abolished the expression of MYC and IRF4 and induced apoptosis, synergistically increases the anti-tumor effect of the individual agents. BRD4 regulates the phosphorylation of CTD Ser2 in vivo. In REC-1 tumor-bearing mice, lenalidomide combined with CPI203 (2.5 mg/kg, I. P.) abolished the expression of MYC and IRF4 and induced apoptosis, synergistically increases the anti-tumor effect of the individual agents. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.501 ml | 12.503 ml | 25.006 ml |
5 mM | 0.5 ml | 2.501 ml | 5.001 ml |
10 mM | 0.25 ml | 1.25 ml | 2.501 ml |
5 mM | 0.05 ml | 0.25 ml | 0.5 ml |