Copanlisib (BAY 80-6946)

For research use only.

Catalog No.S2802

20 publications

Copanlisib (BAY 80-6946) Chemical Structure

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.

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Selleck's Copanlisib (BAY 80-6946) has been cited by 20 publications

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Biological Activity

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.
PI3Kα [1]
(Cell-free assay)
PI3Kδ [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)
PI3Kγ [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Huh7 NVu2RnZjT3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= MUCxNFAhdk1? NIrVeHpEd3Cjbnzpd4ljKGSxc3Wt[IVx\W6mZX70cJkhcW6qaXLpeIVlKGOnbHyg[5Jwf3SqIHnuJJZqfHKxLjDJR|UxRTR5Lkmgcm0v MW[zNFk3Ojl3Mh?=
HepG2 M{nSRmdzd3e2aDDpcohq[mm2b36gZZN{[Xl? NHi2[m0yODBibl2= NHeye|REd3Cjbnzpd4ljKGSxc3Wt[IVx\W6mZX70cJkhcW6qaXLpeIVlKGOnbHyg[5Jwf3SqIHnuJJZqfHKxLjDJR|UxRTNzLk[gcm0v MYKzNFk3Ojl3Mh?=
Hep3B NEKwfGxIem:5dHigbY5pcWKrdH;uJIF{e2G7 NVG2cmZuUUN3ME23Nk41KG6P NWjUNGdjOzB7NkK5OVI>
PLCPRF5 NI\0W5hIem:5dHigbY5pcWKrdH;uJIF{e2G7 MlfWTWM2OD1{OEOgcm0> NUjwWmpjOzB7NkK5OVI>
Chang NWrPc4RZT3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= MmThTWM2OD12NEKgcm0> MVKzNFk3Ojl3Mh?=
JVM-3 MlvvSpVv[3Srb36gZZN{[Xl? M{G2fFQ5KGh? M2XpT4lvcGmkaYTzJI1mfGGkb3zpZ{Bi[3Srdnn0fUB4cXSqIHHuJGlEPTBib3[gNkDPxE1iaX6geIhmKFiWVDDhd5NigQ>? MVmyOVkyOjZ|NR?=
BT-474 NXziT25QTnWwY4Tpc44h[XO|YYm= NVfl[ItFPTBibl2= M2rSflAvPSxiMjygOEwhQCxiMkSgbC=> M{LJeJJieGmmbImgbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHM1PzNuIGSzNFgqKGG|IIflcIwh[XNiaYTzJIRqemWldDDzeYJ{fHKjdHXzJHBTSVN2MDCoWFI1PiliYX7kJGdUUzQQsjCoV|kqNCCjbnSgbY5pcWKrdHnvckB4[XNic4XzeIFqdmWmIH\vdkB2eCC2bzCyOEBpd3W{cx?= MkHqNlQ1OzZyNEi=
SK-BR-3 MUPGeY5kfGmxbjDhd5NigQ>? MVSwMEAyNCB{LDC0JIg> MmHh[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MV[yOFQ{PjB2OB?=
UACC-893 M3XpTGZ2dmO2aX;uJIF{e2G7 NH61eFUxNCBzLDCyMEA1KGh? NWjrPHdT\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NYS2O4U1OjR2M{[wOFg>
HCC-1954 MlfySpVv[3Srb36gZZN{[Xl? M2CxelAtKDFuIEKsJFQhcA>? NUHR[|A3\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MmDzNlQ1OzZyNEi=
MDA-MB-453 M1zyWGZ2dmO2aX;uJIF{e2G7 MWmwMEAyNCB{LDC0JIg> Mk\t[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MVSyOFQ{PjB2OB?=
MDA-MB-361 NWLySoh3TnWwY4Tpc44h[XO|YYm= M16xR|AtKDFuIEKsJFQhcA>? NHGyc5Fld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NFu3W|kzPDR|NkC0PC=>
BT-20 NUDyO4I2TnWwY4Tpc44h[XO|YYm= NHjpdJExNCBzLDCyMEA1KGh? NIjYXnZld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MkLRNlQ1OzZyNEi=
MCF-7 M1zpbWZ2dmO2aX;uJIF{e2G7 NULmRYhHOCxiMTygNkwhPCCq NYnk[Fk2\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NXy4WnM1OjR2M{[wOFg>
T-47D MWPGeY5kfGmxbjDhd5NigQ>? MXqwMEAyNCB{LDC0JIg> M1LDOYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NWXLbI5tOjR2M{[wOFg>
HCC1806 Ml;3SpVv[3Srb36gZZN{[Xl? NXTpUlZxOCxiMTygNkwhPCCq MUfkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? MWWyOFQ{PjB2OB?=
NCI-H292 MVrGeY5kfGmxbjDhd5NigQ>? NFvncWwxNCBzLDCyMEA1KGh? NF7PbYFld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MmK4NlQ1OzZyNEi=
NCI-H1650 M2SwWGZ2dmO2aX;uJIF{e2G7 NH3rOHUxNCBzLDCyMEA1KGh? Mmm1[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MWiyOFQ{PjB2OB?=
CCRF-SB MXzGeY5kfGmxbjDhd5NigQ>? NXzzZ2czOCxiMTygNkwhPCCq NGrPdZRld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NV3OcZBPOjR2M{[wOFg>
U937 NXPuWGJwTnWwY4Tpc44h[XO|YYm= Mn;SNEwhOSxiMjygOEBp MWrkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? MmC3NlQ1OzZyNEi=
SU-DHL-4 MYXGeY5kfGmxbjDhd5NigQ>? M1nQdlAtKDFuIEKsJFQhcA>? NFu3cZBld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MWqyOFQ{PjB2OB?=
SU-DHL-5 MUHGeY5kfGmxbjDhd5NigQ>? NGf5ZVExNCBzLDCyMEA1KGh? Mmfa[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? M3HyVVI1PDN4MES4
HCT116 MlPlSpVv[3Srb36gZZN{[Xl? M{PyNlAtKDFuIEKsJFQhcA>? NYL2WW1{\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= M{K1cVI1PDN4MES4
A549 cells MlW3SpVv[3Srb36gZZN{[Xl? NX:wO4x{OCxiMTygNkwhPCCq Ml3L[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MnrmNlQ1OzZyNEi=
SK-MEL-30 M1[2d2Z2dmO2aX;uJIF{e2G7 M{HIflAtKDFuIEKsJFQhcA>? NETJRXBld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= M3ezSFI1PDN4MES4
SK-MEL-2 cells M{XtR2Z2dmO2aX;uJIF{e2G7 MWOwMEAyNCB{LDC0JIg> M3:zSoRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW M2C2bVI1PDN4MES4
NCI-H1703 NYHsZphITnWwY4Tpc44h[XO|YYm= MkTxNEwhOSxiMjygOEBp MVjkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? M3LHTVI1PDN4MES4
NCI-H661 NX3vVmt{TnWwY4Tpc44h[XO|YYm= MYCwMEAyNCB{LDC0JIg> NVKzfIR4\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NUXVUJc5OjR2M{[wOFg>
PC9 MofMSpVv[3Srb36gZZN{[Xl? M2rselAtKDFuIEKsJFQhcA>? NWrpc4VJ\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NHXYPG4zPDR|NkC0PC=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-AKT / AKT / p-PRAS40(T246) / p-GSK3β(S9) / cleaved caspase-3 / cleaved caspase-7 / PI3K-p85; 

PubMed: 24436048     

BT-474 cells were treated with BAY 80-6946 (50nM) or MK2206 (2μM) and collected at indicated times. Immunoblots of AKT, AKT substrates, and surrogates for apoptosis show similar AKT inhibition but greater apoptosis with PI3K inhibition.

p-FoxO4(T28) / p-S6(S235/236) / p-4E-BP1(S65) / p-4E-BP1(T37/46) / p-HER3(Y1197) / HER3 / p-IGF1Rβ/ IGF1R / p-HER2 / p-EGFR / p-STAT3 / p-ERK; 

PubMed: 24436048     

BT-474 cells were treated with BAY 80-6946 (50nM) or MK2206 (2μM) and collected at indicated times. Immunoblots of AKT and mTOR substrates, RTKs, and parallel pathways like STAT and ERK.

Growth inhibition assay
Cell viability; 

PubMed: 24436048     

BT-474 cells were treated with DMSO, MK2206 (2μM), or BAY 80-6946 (50nM) and viable cells were counted at indicated times, demonstrating loss in viable cell number with PI3K inhibition. Results were reported as a mean of triplicate with standard errors.

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]


Kinase Assay:[1]
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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 Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Rats bearing KPL4 or HCT116 xenografts
  • Dosages: 6 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro 1 mg/mL (2.08 mM)
DMSO 0.002 mg/mL (0.0 mM)
Water 0.002 mg/mL (0.0 mM)

* 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 Information

Molecular Weight 480.52


CAS No. 1032568-63-0
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04042051 Recruiting Drug: Copanlisib|Drug: Trastuzumab emtansine HER2-positive Breast Cancer|Metastatic Breast Cancer|Locally Advanced Breast Cancer|Unresectable Breast Cancer Cancer Trials Ireland November 12 2019 Phase 1
NCT03884998 Recruiting Drug: Copanlisib|Biological: Nivolumab Chronic Lymphocytic Leukemia|Richter Syndrome|Diffuse Large B Cell Lymphoma|Follicular Lymphoma|Indolent Non-hodgkin Lymphoma|Loss of Chromosome 17p|Lymphoplasmacytic Lymphoma|Marginal Zone Lymphoma|TP53 Gene Mutation OHSU Knight Cancer Institute|Oregon Health and Science University|National Cancer Institute (NCI) March 18 2019 Phase 1
NCT03711058 Recruiting Drug: Copanlisib|Drug: Nivolumab 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 January 10 2019 Phase 1|Phase 2

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Frequently Asked Questions

  • Question 1:

    S2802 (BAY 80-6946) has poor solubility in DMSO and water. Do you have any other suggestion to dissolve this chemical?

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID