Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 11,000 | |||
10 mg | 在庫あり | ¥ 16,500 | |||
25 mg | 在庫あり | ¥ 29,500 | |||
50 mg | 在庫あり | ¥ 51,000 | |||
100 mg | 在庫あり | ¥ 85,500 |
説明 | 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. |
ターゲット&IC50 | mTOR:45 nM, PI3Kγ:6.4 nM, PI3Kα:0.5 nM, PI3Kβ:3.7 nM, PI3Kδ:0.7 nM |
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] |
別名 | BAY 80-6946 dihydrochloride |
分子量 | 553.44 |
分子式 | C23H30Cl2N8O4 |
CAS No. | 1402152-13-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 1mg/ml
H2O: 20 mg/mL, Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Copanlisib dihydrochloride 1402152-13-9 Apoptosis PI3K/Akt/mTOR signaling PI3K mTOR Inhibitor antiproliferative inhibit intravenous BAY 80-6946 sub-nanomolar Copanlisib BAY 80-6946 dihydrochloride BAY 80-6946 Dihydrochloride phosphorylation Copanlisib Dihydrochloride Phosphoinositide 3-kinase AKT antitumor administration inhibitor