Copanlisib (BAY 80-6946)

Catalog No.S2802

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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5mg	USD 270	In stock
10mg	USD 370	In stock
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Cited by 1 Publication

Oncotarget, 2016, 7(15):19620-30

PubMed: 26934000

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.

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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]	+ Expand 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)

References

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 Download Copanlisib (BAY 80-6946) SDF

Molecular Weight	480.52
Formula	C₂₃H₂₈N₈O₄
CAS No.	1032568-63-0
Storage	3 years -20°C powder
Synonyms	N/A

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Clinical Trial Information (data from http://clinicaltrials.gov, updated on 2017-02-16)

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.

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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.

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

Selective PI3K Inhibitors

CAL-101 (Idelalisib, GS-1101) p110δ-selective, IC50=2.5 nM.

TGX-221 p110β-specific, IC50=5 nM.
Most Potent PI3K Inhibitor

BEZ235 (NVP-BEZ235, Dactolisib) p110α/γ/δ/β, IC50=4 nM/5 nM/7 nM/75 nM.
FDA-approved PI3K Inhibitor

CAL-101 (Idelalisib, GS-1101) Approved by FDA for Relapsed Chronic Lymphocytic Leukemia, Follicular Lymphoma and Small Lymphocytic Lymphoma.
Newest PI3K Inhibitor

VS-5584 (SB2343) Potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.

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Taselisib (GDC 0032) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with K_i of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

Features:A beta isoform-sparing PI3K inhibitor.
Pilaralisib (XL147) ^New

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LY294002

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3-Methyladenine (3-MA)

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Idelalisib (CAL-101, GS-1101)

Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.
Wortmannin

Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.
Dactolisib (BEZ235, NVP-BEZ235)

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