Copanlisib (BAY 80-6946)

Catalog No.S2802

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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Cited by 13 Publications

3 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. Copanlisib (BAY 80-6946) purchased from Selleck.

  • PI3K inhibitor BAY 80-6946 demonstrated to be effective on ALL-SIL cells,showed an IC50 in the lower micromolar range.

    Dr. Antonino Maria Spartà from University of Bolog. Copanlisib (BAY 80-6946) purchased from Selleck.

  • (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.

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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 M4HZbGdzd3e2aDDpcohq[mm2b36gZZN{[Xl? MYGxNFAhdk1? MlKyR49x[W6uaYPpZkBld3OnLXTldIVv\GWwdHz5JIlvcGmkaYTl[EBk\WyuIHfyc5d1cCCrbjD2bZRzdy5iSVO1NF01Py57IH7NMi=> Mn;pN|A6PjJ7NUK=
HepG2 MVXHdo94fGhiaX7obYJqfG:wIHHzd4F6 MYqxNFAhdk1? MUTDc5Bidmyrc3niJIRwe2VvZHXw[Y5l\W62bImgbY5pcWKrdHXkJINmdGxiZ4Lve5RpKGmwII\peJJwNiCLQ{WwQVMyNjZibl2u MYWzNFk3Ojl3Mh?=
Hep3B M3vE[Gdzd3e2aDDpcohq[mm2b36gZZN{[Xl? M4W1T2lEPTB;N{KuOEBvVQ>? M{P4XlMxQTZ{OUWy
Chang Mk\FS5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? NID6Z49KSzVyPUS0NkBvVQ>? MXKzNFk3Ojl3Mh?=
JVM-3 MX3GeY5kfGmxbjDhd5NigQ>? MkXqOFghcA>? M4\W[IlvcGmkaYTzJI1mfGGkb3zpZ{Bi[3Srdnn0fUB4cXSqIHHuJGlEPTBib3[gNkDPxE1iaX6geIhmKFiWVDDhd5NigQ>? NVrXcmczOjV7MUK2N|U>
BT-474 NFT2S3RHfW6ldHnvckBie3OjeR?= MWi1NEBvVQ>? MlvzNE42NCB{LDC0MEA5NCB{NDDo MmXIdoFxcWSueTDpcohq[mm2czD0bIUheGixc4Doc5J6dGG2aX;uJI9nKEGNVDCoV|Q4OyxiVEOwPEkh[XNid3XscEBieyCrdIOg[Ilz\WO2IIP1ZpN1emG2ZYOgVHJCWzRyIDjUNlQ3MSCjbnSgS3NMO87{IDjTPUktKGGwZDDpcohq[mm2aX;uJJdieyC|dYP0ZYlv\WRiZn;yJJVxKHSxIEK0JIhwfXK| Ml3QNlQ1OzZyNEi=
SK-BR-3 M3LofWZ2dmO2aX;uJIF{e2G7 NWHyU|lTOCxiMTygNkwhPCCq NV34VHps\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MmK0NlQ1OzZyNEi=
UACC-893 NHLjOnpHfW6ldHnvckBie3OjeR?= M3Ha[VAtKDFuIEKsJFQhcA>? NW[zdZVl\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= M4noW|I1PDN4MES4
HCC-1954 NVnITJFqTnWwY4Tpc44h[XO|YYm= MX:wMEAyNCB{LDC0JIg> NV3vRY5S\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NEnlSJIzPDR|NkC0PC=>
MDA-MB-453 M2X3OWZ2dmO2aX;uJIF{e2G7 NU\VbmJFOCxiMTygNkwhPCCq M3XRWIRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NYnSbpJ6OjR2M{[wOFg>
MDA-MB-361 NIDjOXNHfW6ldHnvckBie3OjeR?= MXGwMEAyNCB{LDC0JIg> NUn4Z4c{\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MUmyOFQ{PjB2OB?=
BT-20 NXq1e4JzTnWwY4Tpc44h[XO|YYm= M37JcVAtKDFuIEKsJFQhcA>? NWD2Nm03\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NHTFU5YzPDR|NkC0PC=>
MCF-7 NYH2copQTnWwY4Tpc44h[XO|YYm= NXzMRmZCOCxiMTygNkwhPCCq NWXRU|Jx\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MlfFNlQ1OzZyNEi=
T-47D M{P5U2Z2dmO2aX;uJIF{e2G7 NIPWSmwxNCBzLDCyMEA1KGh? Mnm2[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NWDtRZVbOjR2M{[wOFg>
HCC1806 M3LsPGZ2dmO2aX;uJIF{e2G7 MmPhNEwhOSxiMjygOEBp M4[3fYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MVOyOFQ{PjB2OB?=
NCI-H292 MniySpVv[3Srb36gZZN{[Xl? NG\kWpkxNCBzLDCyMEA1KGh? NEn0WXBld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MW[yOFQ{PjB2OB?=
NCI-H1650 MlzFSpVv[3Srb36gZZN{[Xl? MVSwMEAyNCB{LDC0JIg> NI\Ycplld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NHLpUJQzPDR|NkC0PC=>
CCRF-SB MlzQSpVv[3Srb36gZZN{[Xl? NEDid4kxNCBzLDCyMEA1KGh? MYnkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NX64OmF[OjR2M{[wOFg>
U937 Ml35SpVv[3Srb36gZZN{[Xl? NFHjfWIxNCBzLDCyMEA1KGh? MYDkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NEXJbWUzPDR|NkC0PC=>
SU-DHL-4 M3rTdmZ2dmO2aX;uJIF{e2G7 NU\0WoxlOCxiMTygNkwhPCCq M4TCNYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MV:yOFQ{PjB2OB?=
SU-DHL-5 NWe1d|Z5TnWwY4Tpc44h[XO|YYm= NUf6TXN2OCxiMTygNkwhPCCq NGDQemxld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= M1zIelI1PDN4MES4
HCT116 M4nFdGZ2dmO2aX;uJIF{e2G7 NWPYeFNXOCxiMTygNkwhPCCq M4ezZYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NV\nUY5JOjR2M{[wOFg>
A549 cells MX7GeY5kfGmxbjDhd5NigQ>? M4Tke|AtKDFuIEKsJFQhcA>? NHHaTFlld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NXPVSHZ[OjR2M{[wOFg>
SK-MEL-30 NEj3Z|JHfW6ldHnvckBie3OjeR?= NIWwfnoxNCBzLDCyMEA1KGh? NYGz[nB{\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NWX0SYFSOjR2M{[wOFg>
SK-MEL-2 cells NFTmTnlHfW6ldHnvckBie3OjeR?= MXSwMEAyNCB{LDC0JIg> NYDZVJRV\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NGDBZ3czPDR|NkC0PC=>
NCI-H1703 MXjGeY5kfGmxbjDhd5NigQ>? MU[wMEAyNCB{LDC0JIg> MofI[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NYP0U5JuOjR2M{[wOFg>
NCI-H661 MWjGeY5kfGmxbjDhd5NigQ>? M4XMS|AtKDFuIEKsJFQhcA>? M1rrNoRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MV:yOFQ{PjB2OB?=
PC9 MXPGeY5kfGmxbjDhd5NigQ>? M2THc|AtKDFuIEKsJFQhcA>? NH7STYZld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NIPydFAzPDR|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
  • 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.
    (Only for Reference)

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 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.

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 Not yet recruiting Drug: Copanlisib|Drug: Trastuzumab emtansine HER2-positive Breast Cancer|Metastatic Breast Cancer|Locally Advanced Breast Cancer|Unresectable Breast Cancer Cancer Trials Ireland September 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
NCT03735628 Recruiting Drug: Copanlisib|Drug: Nivolumab Non-small Cell Lung Cancer (NSCLC)|Head and Neck Squamous Cell Carcinoma (HNSCC)|Colorectal Cancer (CRC)|Hepatocellular Carcinoma (HCC) Bayer October 17 2018 Phase 1|Phase 2

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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

  • 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