BAY 80-6946 (Copanlisib)

Catalog No.S2802

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.

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BAY 80-6946 (Copanlisib) Chemical Structure

BAY 80-6946 (Copanlisib) Chemical Structure
Molecular Weight: 480.52

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Product Description

Biological Activity

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.
Targets PI3Kα [1]
(Cell-free assay)
PI3Kδ [1] PI3Kβ [1]
(Cell-free assay)
PI3Kγ [1]
IC50 0.5 nM 0.7 nM 3.7 nM 6.4 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]

Protocol(Only for Reference)

Kinase Assay: [1]

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.

Cell Assay: [1]

Cell lines A series of cancer cell lines
Concentrations ~5 μM
Incubation Time 72 hours
Method Cell proliferation over a 72-hour period is determined using the CellTiter-Glo® luminescent cell viability kit. Briefly, cells are plated in separate microtiter plates. Following an overnight incubation at 37ºC, luminescence values in the t=0 hour plates are determined. Test compounds diluted in growth medium are added to the t=72 hour plates, and the cells are then incubated for 72 hours at 37ºC. Luminescence values are determined with a Wallac 1420 Victor2™ 1420 multilabel HTS counter after a 10-minute reaction with CellTiter-Glo® solution. The percentage inhibition of cell growth is calculated by subtracting the luminescence values in the t=0 hour plates from the corresponding values in the t=72 hour plates. Differences in values between drug-treated cells and controls are used to determine the percentage inhibition of cell growth.

Animal Study: [1]

Animal Models Rats bearing KPL4 or HCT116 xenografts
Formulation PEG400/acidified water (0.1 N HCl, pH 3.5; 20/80, v/v) or 5% mannitol
Dosages 6 mg/kg
Administration i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Liu N, et al. Mol Cancer Ther. 2013, 12(11), 2319-2330.

[2] Elster N, et al. Breast Cancer Res Treat. 2015, 149(2), 373-383.

Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02728258 Not yet recruiting Endometrial Endometrioid Adenocarcinoma|Endometrial Mixed Adenocarcinoma|Endometrial Serous Adenocarcinoma|Endometrial Undifferentiated Carcinoma|M  ...more 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) July 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 Not yet recruiting HER2 Positive Breast Cancer Cancer Trials Ireland April 2016 Phase 1
NCT02626455 Recruiting Lymphoma, Non-Hodgkin Bayer January 2016 Phase 3

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Chemical Information

Download BAY 80-6946 (Copanlisib) SDF
Molecular Weight (MW) 480.52


CAS No. 1032568-63-0
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * 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.
Chemical Name 5-Pyrimidinecarboxamide, 2-amino-N-[2,3-dihydro-7-methoxy-8-[3-(4-morpholinyl)propoxy]imidazo[1,2-c]quinazolin-5-yl]-

Tech Support

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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