Name: Copanlisib
Brand: Selleck Chemicals
SKU: S2802
Rating: 5 (45 reviews)

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

CAS: 1032568-63-0

Selleck's Copanlisib has been cited by 45 publications

Purity & Quality Control

Products often used together with Copanlisib

Darolutamide (ODM-201)

Copanlisib and Darolutamide inhibit the proliferation of prostate cancer models in vitro via strong induction of cell apoptosis and prevention of pro-apoptotic gene down-regulation.

Sugawara T, et al. Cancer Res (2022) 82 (12_Supplement): 651.

Tazemetostat (EPZ-6438)

Copanlisib and Tazemetostat combined use induces a higher expression of PIK3IP1 in Calu3, Sw1573, and all the BEAS2B cell lines.

Chen F, et al. Cancer Lett. 2022 Jan 1;524:151-160.

Anetumab ravtansine

Copanlisib and Anetumab ravtansine combination shows an increase in apoptosis in the OVCAR-3 and OVCAR-8 cell lines.

Quanz M, et al. Oncotarget. 2018 Sep 25; 9(75): 34103–34121.

Venetoclax (ABT-199)

Combining Copanlisib and Venetoclax can induce apoptosis in MCL and MZL cells by downregulating BCL-XL/MCL1 genes.

Tarantelli C, et al. Blood Adv. 2020 Mar 10;4(5):819-829.

Abemaciclib

Copanlisib and Abemaciclib combinatory therapy is effective in overcoming venetoclax resistance in becoming an effective treatment regimen for refractory/relapsed patients in the future.

Che Y, et al. Blood 138 (2021): 2253.

Copanlisib Related Products

Related Targets	p110α p110β p110δ p110γ C2β Vps34	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	Click to Expand

Signaling Pathway

PI3K Signaling Pathway

Choose Selective PI3K Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Kinase Assay	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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
NCT04431635	Active not recruiting	Indolent Lymphoma	University of Michigan Rogel Cancer Center\|Bayer\|Bristol-Myers Squibb\|University of Michigan\|Big Ten Cancer Research Consortium	June 15 2020	Phase 1

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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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