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Copanlisib

Name: Copanlisib
Brand: Selleck Chemicals
SKU: S2802
Rating: 5 (46 reviews)

Synonyms: BAY 80-6946

Catalog No.S2802 Purity: 99.74%

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 46 publications

Purity & Quality Control

Batch: Purity: 99.74%

99.74

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.

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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

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 lnformation & 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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