Copanlisib (Synonyms: BAY 80-6946)

Name: Copanlisib
Brand: MedChemExpress
SKU: HY-15346
Rating: 5.0 (34 reviews)

Cat. No.: HY-15346 Purity: 99.35%: Data Sheet
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Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC₅₀s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.

For research use only. We do not sell to patients.

CAS No. : 1032568-63-0

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 34 publication(s) in Google Scholar

Other Forms of Copanlisib:

Copanlisib dihydrochloride In-stock
Copanlisib (Standard) In-stock

34 Publications Citing Use of MCE Copanlisib

Apoptosis Analysis

RT-PCR

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

: Copanlisib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 30;23(1):215. [Abstract]; Western blot analysis of Akt, p-Akt (Ser473), p-Akt (Thr308), and cleaved caspase 3/8 expression after 6 h of treatment with copanlisib (2 nM, pan-PI3K inhibitor) and GEM treatment.

: Copanlisib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 30;23(1):215. [Abstract]; Colony formation by cells overexpressing cFAM124A after 6 h of treatment with different inhibitors and GEM treatment in 6-well dishes (800 cells/well) for 2 weeks. Each inhibitor, Copanlisib (2 nM, pan-PI3K inhibitor) or K-80003 (5 nM, tRXRα-dependent Akt activation inhibitor).

: Copanlisib purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Sep 30;23(1):215. [Abstract]; Subcutaneous xenograft model of mice in the different groups treated with GEM (40 mg/kg i.p. 2×/week for 4 weeks), Copanlisib (1 mg/kg, iv. 2×/week for 4 weeks), or K-80003 (20 mg/ kg i.p. 2×/week for 4 weeks) at 2 weeks after subcutaneous injection of 5 × 10⁶ cells overexpressing cFAM124A and control cells.

: Copanlisib purchased from MedChemExpress. Usage Cited in: Blood. 2019 Jan 3;133(1):70-80. [Abstract]; Induction of apoptosis after 96-hour exposure to DMSO, Entospletinib (ENTO, 2 μM), Ibrutinib (IBRU, 0.1 μM), Copanlisib (COPA, 0.25 μM), or Pictilisib (PICTI, 0.5 μM) shown as percentage of annexin V/PI-positive cells plus or minus SEM from at least 3 biological replicates.

: Copanlisib purchased from MedChemExpress. Usage Cited in: Blood. 2019 Jan 3;133(1):70-80. [Abstract]; HRK, BCL-xL, BFL-1, or BIM transcript abundance after 24-hour exposure to DMSO, Entospletinib (2 μM), Ibrutinib (0.1 μM), Copanlisib (0.25 μM), or Pictilisib (0.5 μM) was determined with RT-qPCR relative to PPIA.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PI3Kα

0.5 nM (IC₅₀)

PI3Kδ

0.7 nM (IC₅₀)

PI3Kβ

3.7 nM (IC₅₀)

PI3Kγ

6.4 nM (IC₅₀)

mTOR

45 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.12 μM Compound: Copanlisib	Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 32069401]
HCT-116	IC₅₀	0.13 μM Compound: Copanlisib	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method	[PMID: 36586298]
HT-29	IC₅₀	0.93 μM Compound: Copanlisib	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method	[PMID: 36586298]
HT-29	IC₅₀	0.95 μM Compound: Copanlisib	Cytotoxicity against human HT-29 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human HT-29 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 32069401]
HUVEC	IC₅₀	34.75 μM Compound: Copanlisib	Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method	[PMID: 36586298]
HUVEC	IC₅₀	35.42 μM Compound: Copanlisib	Cytotoxicity against HUVEC assessed as reduction in cell viability Cytotoxicity against HUVEC assessed as reduction in cell viability	[PMID: 32069401]
LoVo	IC₅₀	0.053 μM Compound: Copanlisib	Cytotoxicity against human LoVo cells over-expressing HER2 assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human LoVo cells over-expressing HER2 assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 32069401]
LoVo	IC₅₀	0.06 μM Compound: Copanlisib	Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method Antiproliferative activity against human LoVo cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 method	[PMID: 36586298]
MCF7	IC₅₀	0.01 μM Compound: Copanlisib	Cytotoxicity against human MCF7 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human MCF7 cells harboring PIK3CA mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 32069401]

In Vitro

Copanlisib (BAY 80-6946; 20-200 nM; 24 hours; BT20 breast cancer cells) treatmemnt induces apoptosis in a subset of tumor cell lines that are resistant to Lapatinib and Trastuzumab^[1].
Copanlisib (BAY 80-6946; 0.5-500 nM; 2 hours; ELT3 cells) shows complete inhibition of PI3K-mediated AKT phosphorylation in ELT3 cells^[1].
Copanlisib potently inhibits cell proliferation in a panel of human tumor cell lines. Copanlisib has mean IC₅₀ values of 19 nM against cell lines with PIK3CA-activating mutations and 17 nM against HER2-positive cell lines, whereas the activity in PIK3CA wild-type and HER2-negative cells is about 40-fold less potent^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:	BT20 breast cancer cells
Concentration:	20 nM and 62 nM, 200 nM
Incubation Time:	24 hours
Result:	Significantly increased caspase9 activities. Also increased levels of phosphorylated p53 at Ser15and cleaved PARP. Induced caspase-9 activation with an EC₅₀ of 340 nM.

Western Blot Analysis^[1]

Cell Line:	ELT3 cells
Concentration:	0.5 nM, 5 nM, 50 nM, 500 nM
Incubation Time:	2 hours
Result:	Complete inhibition of PI3K-mediated AKT phosphorylation was clearly shown at a concentration of 5 nM.

In Vivo

Copanlisib (BAY 80-6946; 0.5-6 mg/kg; intravenous injection; every second day, every third day; for 60 days; athymic nude rats) treatment displays robust antitumor activity in the rat KPL4 tumor xenograft model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Athymic nude rats injected with KPL4 tumor cells^[1]
Dosage:	0.5 mg/kg, 1 mg/kg, 3 mg/kg or 6 mg/kg
Administration:	Intravenous injection; every second day, every third day; for 60 days
Result:	On day 25, tumor growth inhibition (TGI) rates of 77%, 84%, 99%, and 100% were observed at doses of 0.5, 1, 3, and 6 mg/kg, respectively. All rats remained tumor free at the termination of the study on day 73.

Clinical Trial

Molecular Weight

480.52

Formula

C₂₃H₂₈N₈O₄

CAS No.

1032568-63-0

Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=CN=C(N)N=C1)NC2=NC3=C(OC)C(OCCCN4CCOCC4)=CC=C3C5=NCCN25

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

1 M HCl : 100 mg/mL (208.11 mM; Need ultrasonic)

DMSO : 5 mg/mL (10.41 mM; ultrasonic and adjust pH to 5 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0811 mL	10.4054 mL	20.8108 mL
5 mM	0.4162 mL	2.0811 mL	4.1622 mL
10 mM	0.2081 mL	1.0405 mL	2.0811 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (10.41 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.35%

Select Batch:

Data Sheet (276 KB) SDS (396 KB)

COA (245 KB) HNMR (192 KB) RP-HPLC (257 KB) MS (68 KB) Elemental Analysis Report (103 KB)

Handling Instructions (2659 KB)

References

[1]. Liu N, et al. BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models. Mol Cancer Ther. 2013 Nov;12(11):2319-30. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / 1 M HCl	1 mM	2.0811 mL	10.4054 mL	20.8108 mL	52.0270 mL
	5 mM	0.4162 mL	2.0811 mL	4.1622 mL	10.4054 mL
	10 mM	0.2081 mL	1.0405 mL	2.0811 mL	5.2027 mL
1 M HCl	15 mM	0.1387 mL	0.6937 mL	1.3874 mL	3.4685 mL
	20 mM	0.1041 mL	0.5203 mL	1.0405 mL	2.6013 mL
	25 mM	0.0832 mL	0.4162 mL	0.8324 mL	2.0811 mL
	30 mM	0.0694 mL	0.3468 mL	0.6937 mL	1.7342 mL
	40 mM	0.0520 mL	0.2601 mL	0.5203 mL	1.3007 mL
	50 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0405 mL
	60 mM	0.0347 mL	0.1734 mL	0.3468 mL	0.8671 mL
	80 mM	0.0260 mL	0.1301 mL	0.2601 mL	0.6503 mL
	100 mM	0.0208 mL	0.1041 mL	0.2081 mL	0.5203 mL

Copanlisib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Copanlisib1032568-63-0BAY 80-6946PI3KApoptosisPhosphoinositide 3-kinaseAKTphosphorylationantitumorintravenousadministrationsub-nanomolarantiproliferativeInhibitorinhibitorinhibit

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Copanlisib (Synonyms: BAY 80-6946)

Customer Review

Other Forms of Copanlisib:

Copanlisib Related Antibodies

34 Publications Citing Use of MCE Copanlisib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Copanlisib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Copanlisib Related Classifications

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