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NVS-PAK1-C

Name: NVS-PAK1-C
Brand: TargetMol
SKU: T35928
Rating: 4.5 (1 reviews)

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Catalog No. T35928Cas No. 2250019-95-3

Alias NVS-PAK1-C

NVS-PAK1-1 is a potent allosteric inhibitor of PAK1 with an IC 50 of 5 nM for dephosphorylated PAK1 and 6 nM for phosphorylated PAK1 as assessed. Inhibition is ATP-competitive, most likely due to indirect competition due to incompatibility of ATP binding with the DFG-out binding conformation of the allosteric compound. NVS-PAK1-1 has an IC50 of 270 nM against dephosphorylated PAK2 and 720 nM against phosphorylated PAK2 respectively [1].

NVS-PAK1-C

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Catalog No. T35928Alias NVS-PAK1-CCas No. 2250019-95-3

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$113	35 days	35 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Product Introduction

Bioactivity

Description	NVS-PAK1-1 is a potent allosteric inhibitor of PAK1 with an IC 50 of 5 nM for dephosphorylated PAK1 and 6 nM for phosphorylated PAK1 as assessed. Inhibition is ATP-competitive, most likely due to indirect competition due to incompatibility of ATP binding with the DFG-out binding conformation of the allosteric compound. NVS-PAK1-1 has an IC50 of 270 nM against dephosphorylated PAK2 and 720 nM against phosphorylated PAK2 respectively [1].
Targets&IC50	PAK2:270 nM, PAK1:5 nM, PAK1:0.007 μM (Kd), PAK2:0.4 μM (Kd)
In vitro	NVS-PAK1-1 potently inhibits PAK1 (S144) autophosphorylation at 0.25 μM in the Su86.86 cell line and MEK S289 phosphorylation with an IC 50 =0.21 μM in Su86.86 cells in which PAK2 is downregulated [1].
Synonyms	NVS-PAK1-C

Chemical Properties

Molecular Weight	465.9
Formula	C₂₂H₂₃ClF₃N₅O
Cas No.	2250019-95-3
Smiles	C(C(F)F)N1C=2C(C(N[C@@H]3CN(C(N(C)C)=O)CC3)=NC=4C1=CC=C(F)C4)=CC(Cl)=CC2
Relative Density.	1.42 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: 50 mg/mL (107.32 mM), Sonication is recommended.

DMF: 50 mg/mL (107.32 mM), Sonication is recommended.

Ethanol: 20 mg/mL (42.93 mM), Sonication is recommended.

DMSO:PBS(pH7.2) (1:1): 0.5 mg/mL (1.07 mM), Sonication is recommended.

Solution Preparation Table

Ethanol/DMSO/DMF

	1mg	5mg	10mg	50mg
5 mM	0.4293 mL	2.1464 mL	4.2928 mL	21.4638 mL
10 mM	0.2146 mL	1.0732 mL	2.1464 mL	10.7319 mL
20 mM	0.1073 mL	0.5366 mL	1.0732 mL	5.3660 mL

DMSO/DMF

	1mg	5mg	10mg	50mg
50 mM	0.0429 mL	0.2146 mL	0.4293 mL	2.1464 mL
100 mM	0.0215 mL	0.1073 mL	0.2146 mL	1.0732 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