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Copanlisib dihydrochloride

Name: Copanlisib dihydrochloride
Brand: TargetMol
SKU: T14998
Price: 47 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T14998Cas No. 1402152-13-9

Alias BAY 80-6946 dihydrochloride

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor, with IC50 values of 0.5 nM for PI3Kα, 0.7 nM for PI3Kδ, 3.7 nM for PI3Kβ, and 6.4 nM for PI3Kγ. It exhibits superior antitumor activity and demonstrates more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.

Copanlisib dihydrochloride

🥰Excellent

Purity: 99.16%

Catalog No. T14998Alias BAY 80-6946 dihydrochlorideCas No. 1402152-13-9

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$47	In Stock	In Stock
10 mg	$72	In Stock	In Stock
25 mg	$128	In Stock	In Stock
50 mg	$222	In Stock	In Stock
100 mg	$372	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.16%

Appearance:Solid

Color:White to Yellow

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor, with IC50 values of 0.5 nM for PI3Kα, 0.7 nM for PI3Kδ, 3.7 nM for PI3Kβ, and 6.4 nM for PI3Kγ. It exhibits superior antitumor activity and demonstrates more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.
Targets&IC50	mTOR:45 nM, PI3Kγ:6.4 nM, PI3Kα:0.5 nM, PI3Kβ:3.7 nM, PI3Kδ:0.7 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]
Synonyms	BAY 80-6946 dihydrochloride

Chemical Properties

Molecular Weight	553.44
Formula	C₂₃H₃₀Cl₂N₈O₄
Cas No.	1402152-13-9
Smiles	Cl.Cl.COc1c(OCCCN2CCOCC2)ccc2C3=NCCN3C(NC(=O)c3cnc(N)nc3)=Nc12
Relative Density.	no data available

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 1 mg/mL (1.81 mM), Sonication is recommended.

H2O: 125 mg/mL (225.86 mM), Sonication is recommended.

Solution Preparation Table

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	1.8069 mL	9.0344 mL	18.0688 mL	90.3440 mL

H2O

	1mg	5mg	10mg	50mg
5 mM	0.3614 mL	1.8069 mL	3.6138 mL	18.0688 mL
10 mM	0.1807 mL	0.9034 mL	1.8069 mL	9.0344 mL
20 mM	0.0903 mL	0.4517 mL	0.9034 mL	4.5172 mL
50 mM	0.0361 mL	0.1807 mL	0.3614 mL	1.8069 mL
100 mM	0.0181 mL	0.0903 mL	0.1807 mL	0.9034 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc