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 7 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.
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 M2fybmdzd3e2aDDpcohq[mm2b36gZZN{[Xl? M4\XS|ExOCCwTR?= MXPDc5Bidmyrc3niJIRwe2VvZHXw[Y5l\W62bImgbY5pcWKrdHXkJINmdGxiZ4Lve5RpKGmwII\peJJwNiCLQ{WwQVQ4Njlibl2u MkDlN|A6PjJ7NUK=
HepG2 NXnWPHZoT3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= M{\iW|ExOCCwTR?= NH6y[3REd3Cjbnzpd4ljKGSxc3Wt[IVx\W6mZX70cJkhcW6qaXLpeIVlKGOnbHyg[5Jwf3SqIHnuJJZqfHKxLjDJR|UxRTNzLk[gcm0v MUKzNFk3Ojl3Mh?=
Hep3B NEDyXZZIem:5dHigbY5pcWKrdH;uJIF{e2G7 M1zKemlEPTB;N{KuOEBvVQ>? MUizNFk3Ojl3Mh?=
PLCPRF5 MUPHdo94fGhiaX7obYJqfG:wIHHzd4F6 NH74XnVKSzVyPUK4N{BvVQ>? NHHJeVE{ODl4Mkm1Ni=>
Chang NUTVXIlST3Kxd4ToJIlvcGmkaYTvckBie3OjeR?= MXXJR|UxRTR2MjDuUS=> NH\VT24{ODl4Mkm1Ni=>
JVM-3 NE[wPYdHfW6ldHnvckBie3OjeR?= NVvl[Jd5PDhiaB?= MnPTbY5pcWKrdIOgcYV1[WKxbHnjJIFkfGm4aYT5JJdqfGhiYX6gTWM2OCCxZjCyJO69VSCrbjD0bIUhYFSWIHHzd4F6 MXGyOVkyOjZ|NR?=
BT-474 MYfGeY5kfGmxbjDhd5NigQ>? M3zxN|UxKG6P MmrUNE42NCB{LDC0MEA5NCB{NDDo M1npU5JieGmmbImgbY5pcWKrdIOgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iCDS2SgLHM1PzNuIGSzNFgqKGG|IIflcIwh[XNiaYTzJIRqemWldDDzeYJ{fHKjdHXzJHBTSVN2MDCoWFI1PiliYX7kJGdUUzQQsjCoV|kqNCCjbnSgbY5pcWKrdHnvckB4[XNic4XzeIFqdmWmIH\vdkB2eCC2bzCyOEBpd3W{cx?= M1TXNFI1PDN4MES4
SK-BR-3 M2X2NWZ2dmO2aX;uJIF{e2G7 M3juTlAtKDFuIEKsJFQhcA>? NID0OoJld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MlGzNlQ1OzZyNEi=
UACC-893 MV;GeY5kfGmxbjDhd5NigQ>? NFSzRnYxNCBzLDCyMEA1KGh? M4PEOYRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW M{PGWlI1PDN4MES4
HCC-1954 NFXTW3dHfW6ldHnvckBie3OjeR?= NVq1VJV5OCxiMTygNkwhPCCq NUXScFZv\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= MkXDNlQ1OzZyNEi=
MDA-MB-453 NEnKWWdHfW6ldHnvckBie3OjeR?= M2fkdlAtKDFuIEKsJFQhcA>? NFjzVpBld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= Mn;kNlQ1OzZyNEi=
MDA-MB-361 NVP6fppjTnWwY4Tpc44h[XO|YYm= NIO1fHcxNCBzLDCyMEA1KGh? NYXPSYNm\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NX7QXFdEOjR2M{[wOFg>
BT-20 Mlq0SpVv[3Srb36gZZN{[Xl? MkLRNEwhOSxiMjygOEBp MV7kc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NH\m[pQzPDR|NkC0PC=>
MCF-7 MnuwSpVv[3Srb36gZZN{[Xl? MWGwMEAyNCB{LDC0JIg> MYfkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? NGjaVIYzPDR|NkC0PC=>
T-47D NFnWWYRHfW6ldHnvckBie3OjeR?= MmG4NEwhOSxiMjygOEBp M3jMNoRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW MmLYNlQ1OzZyNEi=
HCC1806 MlT2SpVv[3Srb36gZZN{[Xl? Mo\2NEwhOSxiMjygOEBp NFX2TYpld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NFnXdZAzPDR|NkC0PC=>
NCI-H292 MVLGeY5kfGmxbjDhd5NigQ>? NXvMdpAxOCxiMTygNkwhPCCq MlrC[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NEHVO5UzPDR|NkC0PC=>
NCI-H1650 NY\pbJVMTnWwY4Tpc44h[XO|YYm= MUiwMEAyNCB{LDC0JIg> NFPBb|Rld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= NYfR[nE3OjR2M{[wOFg>
CCRF-SB NWriNYE4TnWwY4Tpc44h[XO|YYm= Ml\VNEwhOSxiMjygOEBp MU\kc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? MX6yOFQ{PjB2OB?=
U937 Mn;CSpVv[3Srb36gZZN{[Xl? NE\ZTnYxNCBzLDCyMEA1KGh? MX;kc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? MnzQNlQ1OzZyNEi=
SU-DHL-4 NFvNcW1HfW6ldHnvckBie3OjeR?= MUmwMEAyNCB{LDC0JIg> M2O5[YRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW M3zYOlI1PDN4MES4
SU-DHL-5 MVzGeY5kfGmxbjDhd5NigQ>? MXywMEAyNCB{LDC0JIg> NXG5fYlb\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NVz2XoRNOjR2M{[wOFg>
HCT116 NYeyUHlrTnWwY4Tpc44h[XO|YYm= MXOwMEAyNCB{LDC0JIg> NVT2[3Bl\G:5boLl[5Vt[XSrb36gc4YhWC2DS2S= NXj0UWdvOjR2M{[wOFg>
A549 cells MUXGeY5kfGmxbjDhd5NigQ>? MX6wMEAyNCB{LDC0JIg> MYPkc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? M4j5V|I1PDN4MES4
SK-MEL-30 M2XnPWZ2dmO2aX;uJIF{e2G7 NVTxfFVwOCxiMTygNkwhPCCq M1rHR4Rwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NYfiblFyOjR2M{[wOFg>
SK-MEL-2 cells M2ezOGZ2dmO2aX;uJIF{e2G7 MWCwMEAyNCB{LDC0JIg> MV7kc5dvemWpdXzheIlwdiCxZjDQMWFMXA>? Mo\uNlQ1OzZyNEi=
NCI-H1703 Ml;HSpVv[3Srb36gZZN{[Xl? NUXRO2t1OCxiMTygNkwhPCCq MkjS[I94dnKnZ4XsZZRqd25ib3[gVE1CU1R? NV7GR4NqOjR2M{[wOFg>
NCI-H661 NYDae5dPTnWwY4Tpc44h[XO|YYm= M4rTTVAtKDFuIEKsJFQhcA>? NFT2TZhld3ewcnXneYxifGmxbjDv[kBRNUGNVB?= MlniNlQ1OzZyNEi=
PC9 NFPnSFRHfW6ldHnvckBie3OjeR?= MYKwMEAyNCB{LDC0JIg> M13reoRwf26{ZXf1cIF1cW:wIH;mJHAuSUuW NWDNd3lQOjR2M{[wOFg>

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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.
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 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