Copanlisib dihydrochloride 是一种选择性和 ATP 竞争性的泛 I 类PI3K抑制剂。它具有优越的抗肿瘤活性，对除 mTOR 以外的其他脂质和蛋白激酶的选择性也超过 2,000 倍。

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 both KPL4 cells and LPA-stimulated PC3 cells, BAY 80-6946 reduces pAKT levels. In a subset of human cancer cell lines with PIK3CA mutations and/or overexpression of HER2, BAY 80-6946 shows antiproliferative activity and induces apoptosis. [1] The combination of HER2-targeted therapies and BAY 80-6946 inhibits growth more effectively than either therapy used alone, and can restore sensitivity to trastuzumab and lapatinib in cells. [2]

In rat KPL4 or HCT116 tumor xenograft model, BAY 80-6946 (6 mg/kg, i.v.) induces 100% complete tumor regression. In nude mice with Lu7860 erlotinib-resistant, patient-derived NSCLC and MAXF1398 patient-derived luminal breast tumor models, BAY 80-6946 (14 mg/kg, i.v.) also causes tumor growth inhibition. [1]

1402152-13-9

C23H30Cl2N8O4

553.45

库潘尼西盐酸;BAY 80-6946 dihydrochloride

H2O:20mg/mL,Need ultrasonic
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years