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Zimlovisertib

Name: Zimlovisertib
Brand: TargetMol
SKU: TQ0167
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0167Cas No. 1817626-54-2

Alias PF-06650833, PF06650833

Zimlovisertib (PF-06650833) is an effective, selective and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) (IC50s: 0.2 and 2.4 nM in the cell and PBMC assay).

Zimlovisertib

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Purity: 98.21%

Catalog No. TQ0167Alias PF-06650833, PF06650833Cas No. 1817626-54-2

Zimlovisertib (PF-06650833) is an effective, selective and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) (IC50s: 0.2 and 2.4 nM in the cell and PBMC assay).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
5 mg	$62	In Stock	In Stock
10 mg	$117	In Stock	In Stock
25 mg	$235	In Stock	In Stock
50 mg	$396	In Stock	In Stock
100 mg	$658	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$67	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:98.21%

Appearance:Solid

Color:White

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COA HPLC HNMR LCMS

Product Introduction

Bioactivity

Description	Zimlovisertib (PF-06650833) is an effective, selective and orally active inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4) (IC50s: 0.2 and 2.4 nM in the cell and PBMC assay).
Targets&IC50	IRAK4:0.2 nM
In vitro	The kinome selectivity profile of PF06650833 (Compound 40) is assessed in a panel of 278 kinases at 200 nM inhibitor concentration using the ATP Km for each kinase. Approximately 100% inhibition is observed for IRAK4. Lactam PF06650833 is assessed in a whole-cell functional VEGF2R assay (PAE-KDR cell line). No activity is observed at concentrations up to and including 30 μM. In a voltage clamp assay, PF06650833 inhibits hERG current by 25% at 100 μM.
In vivo	PF06650833 (0.3-30 mg/kg; p.o; for 2.5 hours; male SD rats) treatment significantly inhibits LPS-induced TNF-α in a dose dependent manner. Mean exposures of PF06650833 in plasma are 2.1 nM, 7.7 nM, 19 nM and 150 nM free, respectively, at 2.5 hours after oral administration of PF06650833 at 0.3, 1, 3, and 30 mg/kg. The fraction unbound in rat plasma of PF06650833 is 0.3.
Animal Research	Animal Model: Male Sprague-Dawley rats. Dosage: 0.1 mg/kg, 1 mg/kg, 3 mg/kg, 30 mg/kg. Administration: Oral administration; for 2.5 hours
Synonyms	PF-06650833, PF06650833

Chemical Properties

Molecular Weight	361.37
Formula	C₁₈H₂₀FN₃O₄
Cas No.	1817626-54-2
Smiles	O(C[C@@H]1[C@H](CC)[C@H](F)C(=O)N1)C=2C3=C(C=C(C(N)=O)C(OC)=C3)C=CN2
Relative Density.	1.34 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: 150 mg/mL (415.09 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (11.07 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	2.7672 mL	13.8362 mL	27.6725 mL	138.3623 mL
5 mM	0.5534 mL	2.7672 mL	5.5345 mL	27.6725 mL
10 mM	0.2767 mL	1.3836 mL	2.7672 mL	13.8362 mL
20 mM	0.1384 mL	0.6918 mL	1.3836 mL	6.9181 mL
50 mM	0.0553 mL	0.2767 mL	0.5534 mL	2.7672 mL
100 mM	0.0277 mL	0.1384 mL	0.2767 mL	1.3836 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