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Trk-IN-4

Name: Trk-IN-4
Brand: TargetMol
SKU: T17169
Rating: 4.5 (1 reviews)

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Catalog No. T17169Cas No. 1799788-94-5

Alias PF-6683324

Trk-IN-4 (PF-6683324) is a potent pan-Trk inhibitor with IC50 = 1.1~2.6 nM for TrkA/TrkB/TrkC and antinociceptive effects. It is also a selective type II PTK6 inhibitor with IC50 = 76 nM and has antitumor effects.

Trk-IN-4

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Purity: 98.13%

Catalog No. T17169Alias PF-6683324Cas No. 1799788-94-5

Product information is being updated, if you want to purchase, please click the bulk custom button.

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Purity:98.13%

Appearance:Solid

Color:White to Yellow

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Product Introduction

Bioactivity

Description	Trk-IN-4 (PF-6683324) is a potent pan-Trk inhibitor with IC50 = 1.1~2.6 nM for TrkA/TrkB/TrkC and antinociceptive effects. It is also a selective type II PTK6 inhibitor with IC50 = 76 nM and has antitumor effects.
Targets&IC50	TrkB:2.6 nM, TrkA:1.9 nM, TrkC:1.1 nM, K+ channel (hERG):14 μM
In vitro	Trk-IN-4 is a potent pan-Trk inhibitor with cellular IC₅₀ values of 1.9 nM (TrkA), 2.6 nM (TrkB), and 1.1 nM (TrkC), showing high kinase selectivity and low hERG liability (IC₅₀ = 14 μM), with favorable lipophilic efficiency (LipE = 5.7)[1].
In vivo	Trk-IN-4 showed significant antinociceptive activity in a rat UV burn hyperalgesia model at oral doses of 0.03-3 mg/kg, with maximal effects at 3 mg/kg. Trk-IN-4 demonstrated good oral bioavailability (52%), low clearance, and peripheral restriction (Cb,u/Cp,u = 0.043), supporting its use as a pain therapeutic with minimal CNS side effects[1].
Synonyms	PF-6683324

Chemical Properties

Molecular Weight	521.46
Formula	C₂₄H₂₃F₄N₅O₄
Cas No.	1799788-94-5
Smiles	O(C1=C(C(N)=O)C=C(C=N1)C=2N=CN(C)C2)[C@@H]3[C@H](F)CN(C(CC4=CC=C(OC(F)(F)F)C=C4)=O)CC3
Relative Density.	1.46 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature,keep away from direct sunlight | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (153.42 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9177 mL	9.5885 mL	19.1769 mL	95.8846 mL
5 mM	0.3835 mL	1.9177 mL	3.8354 mL	19.1769 mL
10 mM	0.1918 mL	0.9588 mL	1.9177 mL	9.5885 mL
20 mM	0.0959 mL	0.4794 mL	0.9588 mL	4.7942 mL
50 mM	0.0384 mL	0.1918 mL	0.3835 mL	1.9177 mL
100 mM	0.0192 mL	0.0959 mL	0.1918 mL	0.9588 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