BAY 80-6946 (Copanlisib)

BAY 80-6946是可逆的PI3K高度选择性抑制剂，对于PI3Kα和β的IC50分别为0.469 nM和3.72 nM。

BAY 80-6946的生物活性

BAY 80-6946(Copanlisib) is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM.
IC50 value: 0.469/3.72 nM(PI3Kα/β) [1]
Target: PI3Kα/β
in vitro: BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. BAY 86-9766 inhibits proliferation with IC50 of 147 nM in HuCCT-1 (KRASG12D ) and 137 nM in EGI-1 (KRASG12D ) cell lines [2].
in vivo: BAY 80-6946 is generally well tolerated through the MTD (maximum tolerated dose) of 0.8 mg/kg. PK (pharmacokinetics) results support weekly dosing. Grade 2/3 hyperglycemia in the first 24 hrs after receiving a dose is common at the MTD. PK, clinical SD and FDG-PET data are consistent with effective exposure and PI3K pathway inhibition [1].