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Copanlisib (BAY 80-6946)
Catalog No.S2802
For research use only.
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.
CAS No. 1032568-63-0
Selleck's Copanlisib (BAY 80-6946) has been cited by 33 publications
Purity & Quality Control
Choose Selective PI3K Inhibitors
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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. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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| 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 (from reference)
| Kinase Assay:[1] |
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| Cell Research:[1] |
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| Animal Research:[1] |
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| References |
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Solubility (25°C)
|
In vitro |
1 mg/mL
(2.08 mM) |
|
| Ethanol |
0.01 mg/mL
(0.02 mM) |
|
| DMSO |
0.002 mg/mL
(0.0 mM) |
Chemical Information
| Molecular Weight | 480.52 | ||
|---|---|---|---|
| Formula | C23H28N8O4 |
||
| CAS No. | 1032568-63-0 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | COC1=C(C=CC2=C3NCCN3C(=NC(=O)C4=CN=C(N=C4)N)N=C21)OCCCN5CCOCC5 | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
mg/kg
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT05082025 | Not yet recruiting | Drug: Copanlisib|Drug: fulvestrant | Endometrial Cancer|Ovarian Cancer | M.D. Anderson Cancer Center|Bayer | February 28 2022 | Phase 2 |
| NCT04939272 | Not yet recruiting | Drug: Copanlisib Hydrochloride|Drug: Venetoclax | Recurrent Mantle Cell Lymphoma|Refractory Mantle Cell Lymphoma | City of Hope Medical Center|National Cancer Institute (NCI) | December 15 2021 | Phase 1|Phase 2 |
| NCT04572763 | Recruiting | Drug: Copanlisib|Drug: Venetoclax | 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 | Recruiting | Drug: Copanlisib | Leukemia Acute Lymphocytic | Dorothy Sipkins MD PhD|Bayer|Duke University | June 21 2021 | Early Phase 1 |
| NCT04431635 | Recruiting | Drug: Copanlisib|Drug: Nivolumab|Drug: Rituximab | Indolent Lymphoma | Big Ten Cancer Research Consortium | June 15 2020 | Phase 1 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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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