Copanlisib (BAY 80-6946)
Molecular Weight(MW): 480.52
Copanlisib (BAY 80-6946) 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.
Cited by 6 Publications
3 Customer Reviews
(A) Total cell lysates were immunoblotted with the indicated antibodies. β-actin served as the loading control.
Oncol Rep, 2017, 37(5):3137-3145. Copanlisib (BAY 80-6946) purchased from Selleck.
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. Copanlisib (BAY 80-6946) purchased from Selleck.
Purity & Quality Control
Choose Selective PI3K Inhibitors
|Description||Copanlisib (BAY 80-6946) 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||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
10% Trifluoroacetic acid water solution
For best results, use promptly after mixing.
* 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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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03586661||Not yet recruiting||Deleterious BRCA1 Gene Mutation|Deleterious BRCA2 Gene Mutation|Endometrial Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Primary Peritoneal High Grade Serous Adenocarcinoma|Recurrent Endometrial Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma||M.D. Anderson Cancer Center|National Cancer Institute (NCI)||February 2019||Phase 1|
|NCT03711058||Not yet recruiting||Unresectable or Metastatic Microsatellite Stable (MSS) Solid Tumor Along With Microsatellite Stable (MSS) Colon Cancer|Colon Cancer||Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Bayer|Bristol-Myers Squibb||November 2018||Phase 1|Phase 2|
|NCT03735628||Not yet recruiting||Non-small Cell Lung Cancer (NSCLC) Head and Neck Squamous Cell Carcinoma (HNSCC) Colorectal Cancer (CRC) Hepatocellular Carcinoma (HCC)||Bayer||October 31 2018||Phase 1|Phase 2|
|NCT03484819||Not yet recruiting||Recurrent Diffuse Large B-Cell Lymphoma|Recurrent Primary Mediastinal (Thymic) Large B-Cell Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma|Refractory Primary Mediastinal (Thymic) Large B-Cell Cell Lymphoma||National Cancer Institute (NCI)||October 19 2018||Phase 2|
|NCT03655301||Recruiting||Healthy Volunteers||Bayer||September 11 2018||Phase 1|
|NCT03581942||Recruiting||Refractory/Recurrent Primary Central Nervous System Lymphoma (PCNSL)||Memorial Sloan Kettering Cancer Center||August 23 2018||Phase 1|Phase 2|
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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Frequently Asked Questions
S2802 (BAY 80-6946) has poor solubility in DMSO and water. Do you have any other suggestion to dissolve this chemical?
We've tested the solubility of S2802 BAY80-6946 in dichloromethane, chloroform, acetonitrile, acetone, tetrahydrofuran and TFA (aq), and finally found it can be dissolved in 10% Trifluoroacetic acid water solution at 1 mg/ml as a clear solution.