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TAK-020

Name: TAK-020
Brand: TargetMol
SKU: T9529
Price: 148 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9529Cas No. 1627603-21-7

TAK-020 is a potent covalent inhibitor of Btk with potential antitumor activity for the study of rheumatoid arthritis and immune-related diseases.

TAK-020

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Purity: 98.66%

Catalog No. T9529Cas No. 1627603-21-7

TAK-020 is a potent covalent inhibitor of Btk with potential antitumor activity for the study of rheumatoid arthritis and immune-related diseases.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$148	In Stock	In Stock
5 mg	$372	In Stock	In Stock
10 mg	$663	In Stock	In Stock
25 mg	$1,370	In Stock	In Stock
50 mg	$2,120	In Stock	In Stock
100 mg	$3,280	-	In Stock
1 mL x 10 mM (in DMSO)	$397	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:98.66%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

TAK-020 AI Summary

TAK-020 exhibits a range of bioactivities, most notably potent inhibition of Btk with an IC50 of less than 1.995 nM and an EC50 of 1.259 nM in human cells. It shows high solubility in various conditions, including <0.1 µg/mL at pH 1.2, <1.1 µg/mL at pH 6.8 in JP2 fluid, and 6.8 µg/mL in GCDC at pH 6.8. The compound demonstrates good apparent permeability in cells with a Papp value of 18.9 nm/s, and moderate metabolic stability in animal liver hepatocytes with extraction ratios ranging from 0.21 to 0.62. It has high plasma protein binding in both rat and human models with PPB values of 90.2% and 88.7% respectively. TAK-020 also displays antiarthritic activity in rat models, inhibiting paw swelling with an ED50 of 0.17 mg/kg. Additionally, it shows inhibitory activity against various kinases (Lck, hERG, Jak3, Blk, BMX, TXK, EGFR, ITK, HER4) and enzymes (PDE3, PDE5, PDE10A2) with varying IC50 values. The compound has low oral bioavailability in rat and dog models (F = 6.0% and 6.5% respectively), though in vivo stability assessments indicate favorable extraction ratios >0.9 and 0.81 in rats and dogs respectively. Stability with glutathione in PBS buffer stands at 75.0%. These properties suggest that TAK-020 has potential therapeutic applications, particularly in arthritis and kinase-related conditions, with considerations for solubility, stability, and metabolism..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

TAK-020 is a potent covalent inhibitor of Btk with potential antitumor activity for the study of rheumatoid arthritis and immune-related diseases.

Chemical Properties

Molecular Weight	351.36
Formula	C₁₈H₁₇N₅O₃
Cas No.	1627603-21-7
Smiles	C=CC(=O)N1CC[C@@H](C1)Oc1nc(cc2ccccc12)-c1nc(=O)[nH][nH]1
Relative Density.	1.47 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 20 mg/mL (56.92 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.85 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8461 mL	14.2304 mL	28.4608 mL	142.3042 mL
5 mM	0.5692 mL	2.8461 mL	5.6922 mL	28.4608 mL
10 mM	0.2846 mL	1.4230 mL	2.8461 mL	14.2304 mL
20 mM	0.1423 mL	0.7115 mL	1.4230 mL	7.1152 mL
50 mM	0.0569 mL	0.2846 mL	0.5692 mL	2.8461 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