Molecular Formula | C23H28N8O4 |
Molar Mass | 480.52 |
Density | 1.51 |
pKa | 8.42±0.20(Predicted) |
Storage Condition | -20℃ |
Physical and Chemical Properties | Bioactive BAY 80-6946 (Copanlisib) is an effective, highly selective, reversible PI3Kα/β inhibitor with an IC50 of 0.469 nM/3.72 nM. Phase 2. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.081 ml | 10.405 ml | 20.811 ml |
5 mM | 0.416 ml | 2.081 ml | 4.162 ml |
10 mM | 0.208 ml | 1.041 ml | 2.081 ml |
5 mM | 0.042 ml | 0.208 ml | 0.416 ml |
in vitro studies
BAY 80-6946 is a PI3K inhibitor with antitumor activity. BAY 86-9766 inhibited the proliferation of HuCCT-1 (KRASG12D) and EGI-1 (KRASG12D) cell lines with IC50 of 147 nM and 137 nM, respectively.
In vivo studies
BAY 80-6946 was well tolerated with an MTD (maximum tolerated dose) of 0.8 mg/kg. The results of PK (pharmacokinetic) studies support weekly administration. Grade 2/3 hyperglycemia occurred during the first 24 hours treated with MTD. PK, clinical SD and FDG-PET data are consistent with effective processing and PI3K pathway inhibition.