1402152-13-9

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity[1].

ChEBI: Copanlisib dihydrochloride is the dihydrochloride salt of copanlisib. It has a role as an antineoplastic agent, an apoptosis inducer and an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor. It contains a copanlisib.

PI3Kα: 0.5 nM (IC₅₀); PI3Kδ: 0.7 nM (IC₅₀); PI3Kβ: 3.7 nM (IC₅₀); PI3Kγ: 6.4 nM (IC₅₀); mTOP: 45 nM (IC₅₀)

[1] Liu N, et al. BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Mol Cancer Ther. 2013 Nov;12(11):2319-30. DOI:10.1158/1535-7163.MCT-12-0993-T