Home PI3K/Akt/mTOR PI3K inhibitor Copanlisib For research use only.

Copanlisib

Synonyms: BAY 80-6946

Copanlisib 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.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!

Copanlisib Chemical Structure

Copanlisib Chemical Structure

CAS No. 1032568-63-0

Purity & Quality Control

Copanlisib Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Huh7 Growth inhibiton assay 100 nM Copanlisib dose-dependently inhibited cell growth in vitro. IC50=47.9 nM. 30962952
HepG2 Growth inhibiton assay 100 nM Copanlisib dose-dependently inhibited cell growth in vitro. IC50=31.6 nM. 30962952
Hep3B Growth inhibiton assay IC50=72.4 nM 30962952
PLCPRF5 Growth inhibiton assay IC50=283 nM 30962952
Chang Growth inhibiton assay IC50=442 nM 30962952
JVM-3 Function assay 48 h inhibits metabolic activity with an IC50 of 2 μM in the XTT assay 25912635
BT-474 Function assay 50 nM 0.5, 2, 4, 8, 24 h rapidly inhibits the phosphorylation of AKT (S473, T308) as well as its direct substrates PRAS40 (T246) and GSK3β (S9), and inhibition was sustained for up to 24 hours 24436048
SK-BR-3 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
UACC-893 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
HCC-1954 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
MDA-MB-453 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
MDA-MB-361 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
BT-20 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
MCF-7 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
T-47D Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
HCC1806 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
NCI-H292 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
NCI-H1650 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
CCRF-SB Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
U937 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
SU-DHL-4 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
SU-DHL-5 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
HCT116 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
A549 cells Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
SK-MEL-30 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
SK-MEL-2 cells Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
NCI-H1703 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
NCI-H661 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
PC9 Function assay 0, 1, 2, 4 h downregulation of P-AKT 24436048
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Copanlisib 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.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
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 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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot 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 p-AKT / AKT / p-PRAS40(T246) / p-GSK3β(S9) / cleaved caspase-3 / cleaved caspase-7 / PI3K-p85 24436048
Growth inhibition assay Cell viability 24436048
In Vivo
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]
Animal Research Animal Models Rats bearing KPL4 or HCT116 xenografts
Dosages 6 mg/kg
Administration i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05082025 Active not recruiting
Endometrial Cancer|Ovarian Cancer
M.D. Anderson Cancer Center|Bayer
 September 27 2022 Phase 2
NCT05217914 Active not recruiting
Relapsed or Refractory Indolent Non-Hodgkin Lymphoma
Bayer
 July 1 2022 --
NCT04939272 Suspended
Recurrent Mantle Cell Lymphoma|Refractory Mantle Cell Lymphoma
City of Hope Medical Center|National Cancer Institute (NCI)
 June 29 2022 Phase 1|Phase 2
NCT04572763 Active not recruiting
Diffuse Large B Cell Lymphoma|Relapsed Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma
Dana-Farber Cancer Institute|AbbVie|Bayer
 September 8 2021 Phase 1|Phase 2
NCT04803123 Terminated
Leukemia Acute Lymphocytic
Dorothy Sipkins MD PhD|Bayer|Duke University
 June 21 2021 Early Phase 1

Chemical Information & Solubility

Molecular Weight 480.52 Formula

C23H28N8O4
CAS No. 1032568-63-0 SDF Download Copanlisib SDF
Smiles COC1=C(C=CC2=C3NCCN3C(=NC(=O)C4=CN=C(N=C4)N)N=C21)OCCCN5CCOCC5
Storage (From the date of receipt)

In vitro
Batch:

5%TFA : 8 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Tech Support

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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