Copanlisib (BAY 80-6946)

Catalog No.S2802

Copanlisib (BAY 80-6946) Chemical Structure

Molecular Weight(MW): 480.52

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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2 Customer Reviews

  • The compounds BAY80-6946 and TG100713, which are respectively an alpha/beta- and a pan-isoforms inhibitors, demonstrated a very good ability to block Jurkat E6.1 proliferation with an IC50 slightly higher than 1 mM.

    Dr. Antonino Maria Spartà from University of Bolog. Copanlisib (BAY 80-6946) purchased from Selleck.

    PI3K inhibitor BAY 80-6946 demonstrated to be effective on ALL-SIL cells,showed an IC50 in the lower micromolar range.

    Dr. Antonino Maria Spartà from University of Bolog. Copanlisib (BAY 80-6946) purchased from Selleck.

Purity & Quality Control

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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.
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 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]

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

Kinase Assay:[1]
+ Expand

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:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Rats bearing KPL4 or HCT116 xenografts
  • Formulation: PEG400/acidified water (0.1 N HCl, pH 3.5; 20/80, v/v) or 5% mannitol
  • Dosages: 6 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro 10% Trifluoroacetic acid water solution 1 mg/mL (2.08 mM)
Ethanol 0.01 mg/mL (0.02 mM)
DMSO 0.002 mg/mL (0.0 mM)
In vivo Add solvents individually and in order:
10% Trifluoroacetic acid water solution
1mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 480.52
Formula

C23H28N8O4

CAS No. 1032568-63-0
Storage powder
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03052933 Not yet recruiting Mature T-Cell and NK-Cell Neoplasm Chonnam National University Hospital|Bayer|Consortium for Improving Survival of Lymphoma May 2017 Phase 1|Phase 2
NCT02728258 Recruiting Endometrial Endometrioid Adenocarcinoma|Endometrial Mixed Adenocarcinoma|Endometrial Serous Adenocarcinoma|Endometrial Undifferentiated Carcinoma|Metastatic Endometrioid Adenocarcinoma|Recurrent Uterine Corpus Carcinoma NRG Oncology|National Cancer Institute (NCI) September 2016 Phase 2
NCT02631590 Recruiting Biliary Carcinoma|Gall Bladder Carcinoma|Cholangiocarcinoma|Gastrointestinal Tumor H. Lee Moffitt Cancer Center and Research Institute|Bayer June 2016 Phase 2
NCT02822482 Recruiting Carcinoma, Squamous Cell of Head and Neck UNICANCER June 2016 Phase 1|Phase 2
NCT02705859 Recruiting HER2 Positive Breast Cancer Cancer Trials Ireland April 2016 Phase 1
NCT02626455 Recruiting Lymphoma, Non-Hodgkin Bayer January 2016 Phase 3

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.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    S2802 (BAY 80-6946) has poor solubility in DMSO and water. Do you have any other suggestion to dissolve this chemical?

  • Answer:

    We've tested the solubility of S2802 BAY80-6946 in dichloromethane, chloroform, acetonitrile, acetone, tetrahydrofuran and TFA (aq), and finally found it can be dissolved in 10% Trifluoroacetic acid water solution at 1 mg/ml as a clear solution.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID