bay-80-6946

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor, with IC50 values of 0.5 nM for PI3Kα, 0.7 nM for PI3Kδ, 3.7 nM for PI3Kβ, and 6.4 nM for PI3Kγ. It exhibits superior antitumor activity and demonstrates more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.

Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents.

7-Methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-amine is a building block.1It has been used in the synthesis of PI3K inhibitors. 1.Scott, W.J., Hentemann, M.F., Rowley, R.B., et al.Discovery and SAR of novel 2,3-dihydroimidazo[1,2-c]quinazoline PI3K inhibitors: Identification of copanlisib (BAY 80-6946)ChemMedChem.11(14)1517-1530(2016)

KT172, a DAGLβ inhibitor, exhibits an IC50 value of 11 nM and has applications in metabolic and inflammatory research.