Copanlisib (BAY 80-6946)

For research use only.

Catalog No.S2802

18 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 18 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.

Purity & Quality Control

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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 Mkn4S5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? MV6xNFAhdk1? M2TWSGNweGGwbHnzbYIh\G:|ZT3k[ZBmdmSnboTsfUBqdmirYnn0[YQh[2WubDDndo94fGhiaX6geol1em9wIFnDOVA:PDdwOTDuUU4> NEfBV|E{ODl4Mkm1Ni=>
HepG2 Mlz4S5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? MnrQNVAxKG6P MX3Dc5Bidmyrc3niJIRwe2VvZHXw[Y5l\W62bImgbY5pcWKrdHXkJINmdGxiZ4Lve5RpKGmwII\peJJwNiCLQ{WwQVMyNjZibl2u NEDhc44{ODl4Mkm1Ni=>
Hep3B NYPaVIZrT3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= NULoVFdbUUN3ME23Nk41KG6P NIK5fXg{ODl4Mkm1Ni=>
PLCPRF5 MULHdo94fGhiaX7obYJqfG:wIHHzd4F6 MYTJR|UxRTJ6MzDuUS=> NFu2Zlk{ODl4Mkm1Ni=>
Chang MmnhS5Jwf3SqIHnubIljcXSxbjDhd5NigQ>? NH71bGFKSzVyPUS0NkBvVQ>? Mn3BN|A6PjJ7NUK=
JVM-3 MoD5SpVv[3Srb36gZZN{[Xl? MXy0PEBp M2q1TIlvcGmkaYTzJI1mfGGkb3zpZ{Bi[3Srdnn0fUB4cXSqIHHuJGlEPTBib3[gNkDPxE1iaX6geIhmKFiWVDDhd5NigQ>? NVjtTXN{OjV7MUK2N|U>
BT-474 NGDtRVFHfW6ldHnvckBie3OjeR?= NYXI[G1UPTBibl2= MWCwMlUtKDJuIESsJFgtKDJ2IHi= NEHSOGNz[XCrZHz5JIlvcGmkaYTzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiQVvUJEhUPDd|LDDUN|A5MSCjczD3[YxtKGG|IHn0d{BlcXKnY4Sgd5Vje3S{YYTld{BRWkGVNECgLHQzPDZrIHHu[EBIW0t|zsKgLHM6MSxiYX7kJIlvcGmkaYTpc44hf2G|IIP1d5RicW6nZDDmc5IhfXBidH:gNlQhcG:3coO= NFO4T3czPDR|NkC0PC=>
SK-BR-3 Ml\VSpVv[3Srb36gZZN{[Xl? NFP0eosxNCBzLDCyMEA1KGh? Mn3O[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MmHsNlQ1OzZyNEi=
UACC-893 NX7DSnNlTnWwY4Tpc44h[XO|YYm= NUTiNldTOCxiMTygNkwhPCCq NGnlTG5ld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MY[yOFQ{PjB2OB?=
HCC-1954 M1HkcGZ2dmO2aX;uJIF{e2G7 NULIdndrOCxiMTygNkwhPCCq MoTY[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NEn1VlIzPDR|NkC0PC=>
MDA-MB-453 MlLSSpVv[3Srb36gZZN{[Xl? NEXjOWMxNCBzLDCyMEA1KGh? NIDKXpRld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NUXSUJo{OjR2M{[wOFg>
MDA-MB-361 M4nSRmZ2dmO2aX;uJIF{e2G7 NWn2dXVWOCxiMTygNkwhPCCq MmS5[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NU\QNop[OjR2M{[wOFg>
BT-20 M3PaV2Z2dmO2aX;uJIF{e2G7 NEjwWWsxNCBzLDCyMEA1KGh? Mnnm[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? M1P0[|I1PDN4MES4
MCF-7 MmXBSpVv[3Srb36gZZN{[Xl? NVjXcFNiOCxiMTygNkwhPCCq NFTDRohld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NHTH[GUzPDR|NkC0PC=>
T-47D MknHSpVv[3Srb36gZZN{[Xl? M1Hs[lAtKDFuIEKsJFQhcA>? NGjp[mpld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= M3PZNVI1PDN4MES4
HCC1806 M4n3OWZ2dmO2aX;uJIF{e2G7 M3\MVlAtKDFuIEKsJFQhcA>? MorY[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? MlHENlQ1OzZyNEi=
NCI-H292 NV7DOm5mTnWwY4Tpc44h[XO|YYm= MkXoNEwhOSxiMjygOEBp M1LVdYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW M2rVZVI1PDN4MES4
NCI-H1650 NX\tOXdrTnWwY4Tpc44h[XO|YYm= MkW2NEwhOSxiMjygOEBp NYXidI5O\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NI\CWoEzPDR|NkC0PC=>
CCRF-SB NX3PNJd2TnWwY4Tpc44h[XO|YYm= MXywMEAyNCB{LDC0JIg> M3j1[oRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW Mle4NlQ1OzZyNEi=
U937 MVrGeY5kfGmxbjDhd5NigQ>? NYDUT2w4OCxiMTygNkwhPCCq NVjxO5VP\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= M2\FdVI1PDN4MES4
SU-DHL-4 NWjQdW9UTnWwY4Tpc44h[XO|YYm= Mn3PNEwhOSxiMjygOEBp NH;Ne2tld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MknoNlQ1OzZyNEi=
SU-DHL-5 NVPVT2hRTnWwY4Tpc44h[XO|YYm= M3LuR|AtKDFuIEKsJFQhcA>? Mlju[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NETWfpkzPDR|NkC0PC=>
HCT116 M3TzVGZ2dmO2aX;uJIF{e2G7 MlvRNEwhOSxiMjygOEBp MoPs[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NFK0TmkzPDR|NkC0PC=>
A549 cells NVL5eGpETnWwY4Tpc44h[XO|YYm= NXjuR4x[OCxiMTygNkwhPCCq MULkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NELlblUzPDR|NkC0PC=>
SK-MEL-30 NWPXTVV{TnWwY4Tpc44h[XO|YYm= MVmwMEAyNCB{LDC0JIg> NWLiVWxW\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NXnBRZd7OjR2M{[wOFg>
SK-MEL-2 cells MUjGeY5kfGmxbjDhd5NigQ>? NUnj[pVDOCxiMTygNkwhPCCq MnLp[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NXrTd2FYOjR2M{[wOFg>
NCI-H1703 NWfCUoFSTnWwY4Tpc44h[XO|YYm= NWHYVYF6OCxiMTygNkwhPCCq NE[zVnpld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MoDyNlQ1OzZyNEi=
NCI-H661 NWj1cnE5TnWwY4Tpc44h[XO|YYm= M3viTVAtKDFuIEKsJFQhcA>? MV3kc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NHXy[VUzPDR|NkC0PC=>
PC9 Mo\sSpVv[3Srb36gZZN{[Xl? NVHS[I04OCxiMTygNkwhPCCq MWLkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NHrZVXYzPDR|NkC0PC=>

... 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]
- Collapse
  • Animal Models: Rats bearing KPL4 or HCT116 xenografts
  • 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.
1mg/mL

* 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

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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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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