Molecular Formula | C21H23F3N6O2
|
Molar Mass | 448.44 |
Density | 1.63±0.1 g/cm3(Predicted) |
Boling Point | 626.4±65.0 °C(Predicted) |
pKa | 15.05±0.40(Predicted) |
Storage Condition | -20℃ |
In vitro study | Human PMBC cells were able to inhibit the production of phosphorylation by phorbol-12-myristate-13-acetate (IC50=1 μm) by CC-930 after stimulation with c-Jun and phyto hemegutinin. CC-930 in 240 kinds of kinase, with significant selectivity. EGFR was the only non-MAP kinase that was inhibited by more than 50% at a concentration of 3 μm CC-930 (IC50=0.38 μm). At the concentration of 10 μm, the inhibitory effect of CC-930 on 75 receptors, ion channels and neurotransmitter transporters was not more than 50%. The inhibitory effect of CC-930 on CYP450 enzymes is not significant, and metabolism occurs under the action of CYP3A4 and 2D6. |
In vivo study | In an acute PK-PD rat model of LPS-induced TNFα production, the in vivo TNFα production was reduced by 23% and 77% at 10 mg/kg and 30 mg/kg of CC-930, respectively, orally. CC-930 is well tolerated in vivo, and its effect is proportional to the dose. |