Copanlisib dihydrochloride

Copanlisib dihydrochloride is an ATP-competitive pan-class I PI3K inhibitor (IC50s: 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ) . Copanlisib dihydrochloride has superior antitumor activity and it also has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. (In Vitro) :Copanlisib (BAY 80-6946; 20-200 nM; 24 hours; BT20 breast cancer cells) treatmemnt induces apoptosis in a subset of tumor cell lines that are resistant to Lapatinib and Trastuzumab.Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hours; ELT3 cells) treatmemnt shows complete inhibition of PI3K-mediated AKT phosphorylation in ELT3 cells. Copanlisib potently inhibits cell proliferation in a panel of human tumor cell lines. Copanlisib has mean IC50 values of 19 nM against cell lines with PIK3CA-activating mutations and 17 nM against HER2-positive cell lines, whereas the activity in PIK3CA wild-type and HER2-negative cells is about 40-fold less potent. (In Vivo) :Copanlisib (BAY 80-6946; 0.5-6 mg/kg; intravenous injection; every second day, every third day; for 60 days; athymic nude rats) treatment displays robust antitumor activity in the rat KPL4 tumor xenograft model.

1402152-13-9

BAY 80-6946 dihydrochloride

Pharmacology & Drug Discovery

>98% (HPLC)

DMSO:10 mM

O=C (C1=CN=C (N) N=C1) NC2=NC3=C (C=CC (OCCCN4CCOCC4) =C3OC) C5=NCCN25.[H]Cl.[H]Cl

C23H30Cl2N8O4

553.44

Storage temperature: -20°C. Stability: ≥ 2 years