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BTK inhibitor 17

Name: BTK inhibitor 17
Brand: TargetMol
SKU: T9706
Price: 86 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9706Cas No. 1858206-76-4

BTK inhibitor 17 is a potent irreversible Bruton's tyrosine kinase (BTK) inhibitor with an IC50 value of 2.1 nM, suitable for use in rheumatoid arthritis studies.

BTK inhibitor 17

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Purity: 99.88%

Catalog No. T9706Cas No. 1858206-76-4

BTK inhibitor 17 is a potent irreversible Bruton's tyrosine kinase (BTK) inhibitor with an IC50 value of 2.1 nM, suitable for use in rheumatoid arthritis studies.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$86	In Stock	In Stock
5 mg	$178	In Stock	In Stock
10 mg	$278	In Stock	In Stock
25 mg	$447	In Stock	In Stock
50 mg	$592	In Stock	In Stock
100 mg	$828	In Stock	In Stock
200 mg	$1,090	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$178	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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Purity:99.88%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	BTK inhibitor 17 is a potent irreversible Bruton's tyrosine kinase (BTK) inhibitor with an IC50 value of 2.1 nM, suitable for use in rheumatoid arthritis studies.
Targets&IC50	BTK:2.1 nM
In vitro	BTK inhibitor 17 exhibited high potency against BTK kinase and acceptable PK profile. BTK inhibitor 17 could covalently bind to Cys481 and formed an HB network with gatekeeper Thr474, hinge key residues Met477 and Glu475[1].
In vivo	BTK inhibitor 17 demonstrated significant in vivo efficacy in a mouse-collagen-induced arthritis (CIA) model. BTK inhibitor 17 shows >95% plasma protein binding across three species of human, rat, and mouse. After an intravenous injection, the half-life (rat, 0.32 h; mice, 0.42 h), clearance (rat, 54.6 mL/min/kg; mice, 31.3 mL/min/kg), volume of distribution (rat, 1.55 L/kg; mice, 0.82 L/kg), and AUC exposure (rat, 604 ng.h/mL; mice, 576 ng.h/mL) are observed in two species. After oral administration, BTK inhibitor 17 exhibits higher Cmax (rat, 466 ng/mL; mice, 252 ng/mL) and plasma exposure (rat, 642 ng.h/mL; mice, 128 ng.h/mL) with a favorable oral bioavailability (rat, 23.7%; mice, 11.2%)[1]. In male Balb/C mice injected with collagen, BTK inhibitor 17 inhibited the significant progression of the disease and exhibited a clear dose-dependent reduction per paw clinical scores[1].

Chemical Properties

Molecular Weight	456.5
Formula	C₂₅H₂₄N₆O₃
Cas No.	1858206-76-4
Smiles	Nc1n[nH]c(=O)c2n(nc(-c3ccc(Oc4ccccc4)cc3)c12)[C@@H]1CCCN(C1)C(=O)C=C
Relative Density.	1.40 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: 100 mg/mL (219.06 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.76 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	2.1906 mL	10.9529 mL	21.9058 mL	109.5290 mL
5 mM	0.4381 mL	2.1906 mL	4.3812 mL	21.9058 mL
10 mM	0.2191 mL	1.0953 mL	2.1906 mL	10.9529 mL
20 mM	0.1095 mL	0.5476 mL	1.0953 mL	5.4765 mL
50 mM	0.0438 mL	0.2191 mL	0.4381 mL	2.1906 mL
100 mM	0.0219 mL	0.1095 mL	0.2191 mL	1.0953 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