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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $47 | In Stock | |
10 mg | $72 | In Stock | |
25 mg | $128 | In Stock | |
50 mg | $222 | In Stock | |
100 mg | $372 | In Stock |
Description | Copanlisib dihydrochloride (BAY 80-6946 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 | 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 vivo | 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] |
Alias | BAY 80-6946 dihydrochloride |
Molecular Weight | 553.44 |
Formula | C23H30Cl2N8O4 |
Cas No. | 1402152-13-9 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility Information | DMSO: 1mg/ml ![]() H2O: 20 mg/mL |
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