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PRN694

Name: PRN694
Brand: TargetMol
SKU: T16578
Rating: 4.5 (1 reviews)

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Catalog No. T16578Cas No. 1575818-46-0

PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor (IC50s: 0.3 nM and 1.4 nM, respectively).

PRN694

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Catalog No. T16578Cas No. 1575818-46-0

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$2,810	3-6 months	3-6 months
50 mg	$3,850	3-6 months	3-6 months
100 mg	$5,070	3-6 months	3-6 months

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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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Product Introduction

Bioactivity

Description	PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor (IC50s: 0.3 nM and 1.4 nM, respectively).
Targets&IC50	BTK:17 nM, RLK:1.4 nM, BLK:125 nM, BMX?kinase:17 nM, JAK3:30 nM, ITK:0.3 nM, TEC:3.3 nM
In vitro	PRN694 obviously decreases NK cell FcR-induced killing at concentrations exceeding 0.37 μM. PRN694 inhibits TEC, BTK, BMX, BLK, JAK3 with IC50s of 3.3, 17, 17, 125, 30 nM, respectively. Immunoblot analysis of TCR activation pathways shows that PRN694 blocks activation or nuclear translocation of NFAT1, JunB, pIκBα, and pERK. Results display inhibition of Ca2+ signaling with PRN694 at all concentrations above 1 nM. Day 6 flow cytometry analysis reveals that PRN694 significantly inhibits the anti-CD3/CD28-induced proliferation of both CD4 and CD8 T-cells (p<0.01)[1].
In vivo	RN694 treatment also causes obviously lower weights relative to the vehicle (p<0.05). Colitis studies show reduced numbers of CD4+ T cells present in the colonic epithelium of PRN694-treated mice compare with controls. The PRN694 occupancy of ITK is 98, 95, and 54% at 1, 6, and 14 h, respectively. The concentrations of PRN694 in the plasma are 2.8, 0.66, and 0.027 μM at 1, 6, and 14 h, respectively. At 14 h, the plasma level of PRN694 is over 10 fold lower than the IC50 in whole blood [1][2].

Chemical Properties

Molecular Weight	543.67
Formula	C₂₈H₃₅F₂N₅O₂S
Cas No.	1575818-46-0
Smiles	C[C@H](NCc1ccc2n(C[C@H]3CCCN3C(=O)C=C)c(NC(=O)c3ccc(s3)C(F)F)nc2c1)C(C)(C)C
Relative Density.	1.29 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: 125 mg/mL (229.92 mM), Sonication and heating are recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.07 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	1.8394 mL	9.1968 mL	18.3935 mL	91.9676 mL
5 mM	0.3679 mL	1.8394 mL	3.6787 mL	18.3935 mL
10 mM	0.1839 mL	0.9197 mL	1.8394 mL	9.1968 mL
20 mM	0.0920 mL	0.4598 mL	0.9197 mL	4.5984 mL
50 mM	0.0368 mL	0.1839 mL	0.3679 mL	1.8394 mL
100 mM	0.0184 mL	0.0920 mL	0.1839 mL	0.9197 mL

Calculator

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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