Molecular Formula | C18H17ClN4O |
Molar Mass | 340.81 |
Density | 1.373±0.06 g/cm3(Predicted) |
Boling Point | 576.5±50.0 °C(Predicted) |
pKa | 9.65±0.40(Predicted) |
Storage Condition | -20℃ |
In vitro study | MSC2530818 binds CDK8 and CDK19 with approximate affinity, effectively inhibiting phospho-STAT1 in SW620 colorectal cancer cells. |
In vivo study | MSC2530818 had acceptable, good pharmacokinetic properties in all animal species tested (mouse, rat, canine). In human SW620 colorectal cancer xenograft model, can effectively reduce the tumor growth rate. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.934 ml | 14.671 ml | 29.342 ml |
5 mM | 0.587 ml | 2.934 ml | 5.868 ml |
10 mM | 0.293 ml | 1.467 ml | 2.934 ml |
5 mM | 0.059 ml | 0.293 ml | 0.587 ml |
biological activity | MSC2530818 is a CDK8 inhibitor with IC50 of 2.6 nM. It has good kinase selectivity, biochemical and cellular potency, microsomal stability, and biological oral activity. |
target | TargetValue CDK8 (Cell-free say) 2.6 nM |
Target | Value |
CDK8 (Cell-free assay) | 2.6 nM |
in vitro study | MSC2530818 binds CDK8 and CDK19 with approximate affinity, effectively inhibiting phospho-STAT1 in SW620 colorectal cancer cells. |
in vivo studies | MSC2530818 have acceptable and good pharmacokinetic properties in all animal species tested (mice, rats, dogs). In the human SW620 colorectal cancer transplanted tumor model, it can effectively reduce the tumor growth rate. |