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Poseltinib

Name: Poseltinib
Brand: TargetMol
SKU: T4413
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4413Cas No. 1353552-97-2

Alias LY3337641, LY 3337641, HM71224, HM 71224

Poseltinib is an orally active, selective, and irreversible inhibitor of Bruton's tyrosine kinase (BTK), with an IC50 value of 1.95 nM. Poseltinib demonstrates 0.3-, 2.3-, and 2.4-fold higher selectivity for BTK over BMX, TEC, and TXK, respectively. Poseltinib covalently binds to cysteine 481 in BTK’s active site, thereby inhibiting BCR-, FcR-, and TLR-mediated signaling pathways.

Poseltinib

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Purity: 99.98%

Catalog No. T4413Alias LY3337641, LY 3337641, HM71224, HM 71224Cas No. 1353552-97-2

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$30	In Stock	In Stock
5 mg	$44	In Stock	In Stock
10 mg	$73	In Stock	In Stock
25 mg	$157	In Stock	In Stock
50 mg	$289	In Stock	In Stock
100 mg	$455	-	In Stock
200 mg	$655	-	In Stock
1 mL x 10 mM (in DMSO)	$45	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:99.98%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Poseltinib is an orally active, selective, and irreversible inhibitor of Bruton's tyrosine kinase (BTK), with an IC50 value of 1.95 nM. Poseltinib demonstrates 0.3-, 2.3-, and 2.4-fold higher selectivity for BTK over BMX, TEC, and TXK, respectively. Poseltinib covalently binds to cysteine 481 in BTK’s active site, thereby inhibiting BCR-, FcR-, and TLR-mediated signaling pathways.
Targets&IC50	BTK:1.95 nM
In vitro	Methods: Ramos B lymphoma cells of Homo sapiens were treated with Poseltinib (0.1-100 nM, 30 min), and the expression of related proteins was analyzed by Western Blot. Results: Poseltinib simultaneously blocked the autophosphorylation of BTK and the phosphorylation of its physiological substrate PLCγ2, with IC50 values both less than 10 nM. [1]
In vivo	Methods: Poseltinib (3-30 mg/kg, daily) was orally administered to MRL/lpr and NZB/W F1 mouse models to evaluate the therapeutic effects of Poseltinib on systemic lupus erythematosus (SLE)-like disease characteristics in mice. Results: By inhibiting BTK, Poseltinib effectively reduced the overactivation of B cells and the production of autoantibodies, significantly alleviating the progression of SLE and lupus nephritis (LN) in mice. Poseltinib demonstrated notable improvements in skin lesions, renal function, kidney injury, and inflammation, while also increasing survival rates. [1]
Synonyms	LY3337641, LY 3337641, HM71224, HM 71224

Chemical Properties

Molecular Weight	470.52
Formula	C₂₆H₂₆N₆O₃
Cas No.	1353552-97-2
Smiles	O=C(C=C)NC=1C=CC=C(OC2=NC(=NC=3C=COC23)NC4=CC=C(C=C4)N5CCN(C)CC5)C1
Relative Density.	1.316 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: 80 mg/mL (170.02 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1253 mL	10.6265 mL	21.2531 mL	106.2654 mL
5 mM	0.4251 mL	2.1253 mL	4.2506 mL	21.2531 mL
10 mM	0.2125 mL	1.0627 mL	2.1253 mL	10.6265 mL
20 mM	0.1063 mL	0.5313 mL	1.0627 mL	5.3133 mL
50 mM	0.0425 mL	0.2125 mL	0.4251 mL	2.1253 mL
100 mM	0.0213 mL	0.1063 mL	0.2125 mL	1.0627 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