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.
Targets
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
JVM-3 NWrSSYZITnWwY4Tpc44h[XO|YYm= NFjBc2I1QCCq MkDmbY5pcWKrdIOgcYV1[WKxbHnjJIFkfGm4aYT5JJdqfGhiYX6gTWM2OCCxZjCyJO69VSCrbjD0bIUhYFSWIHHzd4F6 NVTFbmF1OjV7MUK2N|U>
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=
HCC1806 M4K4VGZ2dmO2aX;uJIF{e2G7 MWSwMEAyNCB{LDC0JIg> M2nWTYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MkDwNlQ1OzZyNEi=
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
Assay
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.

24436048
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.

24436048
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

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
Formula

C23H28N8O4
CAS No. 1032568-63-0
Storage powder
in solvent
Synonyms N/A
Smiles COC1=C(C=CC2=C3NCCN3C(=NC(=O)C4=CN=C(N=C4)N)N=C21)OCCCN5CCOCC5

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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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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