BAY 80-6946 (Copanlisib)
Molecular Weight(MW): 480.52
BAY 80-6946 (Copanlisib) is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.
2 Customer Reviews
The compounds BAY80-6946 and TG100713, which are respectively an alpha/beta- and a pan-isoforms inhibitors, demonstrated a very good ability to block Jurkat E6.1 proliferation with an IC50 slightly higher than 1 mM.
Dr. Antonino Maria Spartà from University of Bolog. BAY 80-6946 (Copanlisib) purchased from Selleck.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
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|Description||BAY 80-6946 (Copanlisib) is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.|
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.  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. 
|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. |
Biochemical lipid kinase assays:The effect of BAY 80-6946 on PI3Kα, PI3Kβ, and PI3Kγ activity is measured by the inhibition of 33P incorporation into phosphatidylinositol (PI) in 384-well MaxiSorp® plates coated with 2 µg/well of PI and phosphatidylserine (PS) (1:1 molar ratio). In each PI3K isoform assay, 9 µL of reaction buffer (50 mM MOPSO, pH 7.0, 100 mM NaCl, 4 mM MgCl2, 0.1% BSA) containing 7.5 ng of His-tagged N-terminal truncated p110α or p110β protein, or 25 ng of purified human p110γ protein, is used. The reaction is started by adding 5 µL of a 40-µM ATP solution containing 20 µCi/mL [33>/sup>P]-ATP. After 2 hours incubation at room temperature, the reaction is terminated by addition of 5 µL of a 25-mM EDTA solution. The plates are washed and Ultima Gold™ scintillation cocktail (25 µL) is then added. The radioactivity incorporated into the immobilized PI substrate is determined with a BetaPlate Liquid Scintillation Counter.
|In vitro||10% Trifluoroacetic acid water solution||1 mg/mL (2.08 mM)|
|Ethanol||0.01 mg/mL (0.02 mM)|
|DMSO||0.002 mg/mL (0.0 mM)|
|In vivo||10% Trifluoroacetic acid water solution||1mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03052933||Not yet recruiting||Mature T-Cell and NK-Cell Neoplasm||Chonnam National University Hospital|Bayer|Consortium for Improving Survival of Lymphoma||May 2017||Phase 1|Phase 2|
|NCT02728258||Recruiting||Endometrial Endometrioid Adenocarcinoma|Endometrial Mixed Adenocarcinoma|Endometrial Serous Adenocarcinoma|Endometrial Undifferentiated Carcinoma|Metastatic Endometrioid Adenocarcinoma|Recurrent Uterine Corpus Carcinoma||NRG Oncology|National Cancer Institute (NCI)||September 2016||Phase 2|
|NCT02631590||Recruiting||Biliary Carcinoma|Gall Bladder Carcinoma|Cholangiocarcinoma|Gastrointestinal Tumor||H. Lee Moffitt Cancer Center and Research Institute|Bayer||June 2016||Phase 2|
|NCT02822482||Recruiting||Carcinoma, Squamous Cell of Head and Neck||UNICANCER||June 2016||Phase 1|Phase 2|
|NCT02705859||Recruiting||HER2 Positive Breast Cancer||Cancer Trials Ireland||April 2016||Phase 1|
|NCT02626455||Recruiting||Lymphoma, Non-Hodgkin||Bayer||January 2016||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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