Copanlisib (BAY 80-6946)

For research use only.

Catalog No.S2802

20 publications

Copanlisib (BAY 80-6946) Chemical Structure

CAS No. 1032568-63-0

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 MVXHdo94fGhiaX7obYJqfG:wIHHzd4F6 M1HqdVExOCCwTR?= NXvEWoVzS2:yYX7sbZNq[iCmb4PlMYRmeGWwZHXueIx6KGmwaHnibZRm\CClZXzsJIdzd3e2aDDpckB3cXS{bz6gTWM2OD12Nz65JI5ONg>? MnPBN|A6PjJ7NUK=
HepG2 MVXHdo94fGhiaX7obYJqfG:wIHHzd4F6 NGrqPFkyODBibl2= MV;Dc5Bidmyrc3niJIRwe2VvZHXw[Y5l\W62bImgbY5pcWKrdHXkJINmdGxiZ4Lve5RpKGmwII\peJJwNiCLQ{WwQVMyNjZibl2u M3\3RlMxQTZ{OUWy
Hep3B NESzdHNIem:5dHigbY5pcWKrdH;uJIF{e2G7 MkXUTWM2OD15Mj60JI5O NY\1XJZPOzB7NkK5OVI>
PLCPRF5 NWfn[4xpT3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= NWe5XVUzUUN3ME2yPFMhdk1? MnfLN|A6PjJ7NUK=
Chang NUC2OJBRT3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= MXPJR|UxRTR2MjDuUS=> M4jpWlMxQTZ{OUWy
BT-474 NEPlc2hHfW6ldHnvckBie3OjeR?= Moj0OVAhdk1? NV;CV3NbOC53LDCyMEA1NCB6LDCyOEBp NVnheVE1emGyaXTsfUBqdmirYnn0d{B1cGVicHjvd5Bpd3K7bHH0bY9vKG:oIFHLWEApWzR5MzygWFMxQCliYYOge4VtdCCjczDpeJMh\Gm{ZXP0JJN2[nO2cnH0[ZMhWFKDU{SwJEhVOjR4KTDhcoQhT1ONM98yJEhUQSluIHHu[EBqdmirYnn0bY9vKHejczDzeZN1[WmwZXSg[o9zKHWyIITvJFI1KGixdYLz M3ziblI1PDN4MES4
SK-BR-3 NYPZeWUzTnWwY4Tpc44h[XO|YYm= MmG3NEwhOSxiMjygOEBp M3\YVYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MX6yOFQ{PjB2OB?=
UACC-893 MnjQSpVv[3Srb36gZZN{[Xl? M37ZTVAtKDFuIEKsJFQhcA>? NVnhRXVt\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MV2yOFQ{PjB2OB?=
HCC-1954 NFqw[WlHfW6ldHnvckBie3OjeR?= MkKwNEwhOSxiMjygOEBp NV7kVmRy\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MXeyOFQ{PjB2OB?=
MDA-MB-453 M1HE[mZ2dmO2aX;uJIF{e2G7 MoruNEwhOSxiMjygOEBp NEjzO2Zld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NEjWdGUzPDR|NkC0PC=>
MDA-MB-361 M3n2V2Z2dmO2aX;uJIF{e2G7 NEfifXgxNCBzLDCyMEA1KGh? NUjjOVZ6\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= M3fq[|I1PDN4MES4
BT-20 M{\HcWZ2dmO2aX;uJIF{e2G7 M3v1TFAtKDFuIEKsJFQhcA>? M4jhSIRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW M3foVVI1PDN4MES4
MCF-7 MYrGeY5kfGmxbjDhd5NigQ>? NVeyVYF3OCxiMTygNkwhPCCq M3z2RoRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NWDHTGlxOjR2M{[wOFg>
T-47D MnjiSpVv[3Srb36gZZN{[Xl? MUmwMEAyNCB{LDC0JIg> NVm2VZZk\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MlPwNlQ1OzZyNEi=
NCI-H292 MV;GeY5kfGmxbjDhd5NigQ>? NFH0V3kxNCBzLDCyMEA1KGh? M{LYPIRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NEWwSYczPDR|NkC0PC=>
NCI-H1650 MUTGeY5kfGmxbjDhd5NigQ>? Mln5NEwhOSxiMjygOEBp NXvvXJUz\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= M2PjTFI1PDN4MES4
CCRF-SB NGX6UmdHfW6ldHnvckBie3OjeR?= NHL2ZYExNCBzLDCyMEA1KGh? NYjGc2R7\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MmLGNlQ1OzZyNEi=
U937 M17UO2Z2dmO2aX;uJIF{e2G7 NVvufndLOCxiMTygNkwhPCCq MX3kc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? M1HiXlI1PDN4MES4
SU-DHL-4 MVnGeY5kfGmxbjDhd5NigQ>? MXewMEAyNCB{LDC0JIg> NVXpTIN[\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MUOyOFQ{PjB2OB?=
SU-DHL-5 MX;GeY5kfGmxbjDhd5NigQ>? MlTzNEwhOSxiMjygOEBp NWLUbW97\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NGC3XmgzPDR|NkC0PC=>
HCT116 M1zqUmZ2dmO2aX;uJIF{e2G7 MUewMEAyNCB{LDC0JIg> NFnyZ49ld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MVWyOFQ{PjB2OB?=
A549 cells NYDTSo5YTnWwY4Tpc44h[XO|YYm= NV[4Z4JxOCxiMTygNkwhPCCq MoP4[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MUeyOFQ{PjB2OB?=
SK-MEL-30 NX7QWG9lTnWwY4Tpc44h[XO|YYm= Mle4NEwhOSxiMjygOEBp M2HXeYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MWiyOFQ{PjB2OB?=
SK-MEL-2 cells M2jXUmZ2dmO2aX;uJIF{e2G7 NFHCfWIxNCBzLDCyMEA1KGh? NXXzR|NT\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NEXaWm4zPDR|NkC0PC=>
NCI-H1703 MoPNSpVv[3Srb36gZZN{[Xl? M1TkVFAtKDFuIEKsJFQhcA>? NFy4bppld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MVyyOFQ{PjB2OB?=
NCI-H661 NUPUU2p6TnWwY4Tpc44h[XO|YYm= NWfqUodjOCxiMTygNkwhPCCq M13GbYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MmWwNlQ1OzZyNEi=
PC9 NI\oSopHfW6ldHnvckBie3OjeR?= M3j4cVAtKDFuIEKsJFQhcA>? NEP6WJlld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= M4L5XVI1PDN4MES4

... 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
NCT04431635 Recruiting Drug: Copanlisib|Drug: Nivolumab|Drug: Rituximab Indolent Lymphoma Big Ten Cancer Research Consortium June 15 2020 Phase 1
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

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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