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NVS-PAK1-1

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Purity:99.74%

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COA HPLC HNMR

NVS-PAK1-1

Catalog No. T16367Cas No. 1783816-74-9

NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).

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Pack Size	Price	Availability
1 mg	$44	In Stock
5 mg	$97	In Stock
10 mg	$177	In Stock
25 mg	$387	In Stock
50 mg	$579	In Stock
100 mg	$828	In Stock
1 mL x 10 mM (in DMSO)	$97	In Stock

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Product Introduction

Bioactivity

Description	NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).
In vitro	NVS-PAK1-1 inhibits the proliferation of the Su86.86 cell line only above a concentration of 2 μM, consistent with the observation. NVS-PAK1-1 (6-20 μM) inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Inhibition of downstream signaling, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, and cell proliferation at a significantly lower 0.21 μM concentration is achieved. NVS-PAK1-1 shows high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 displays excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases .
In vivo	NVS-PAK1-1 displays relatively poor stability in rat liver microsomes (RLM). This would limit its application for in vivo studies (t1/2 in RLM 3.5 min).

Chemical Properties

Molecular Weight	479.93
Formula	C23H25ClF3N5O
Cas No.	1783816-74-9

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (260.45 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0836 mL	10.4182 mL	20.8364 mL	104.1819 mL
5 mM	0.4167 mL	2.0836 mL	4.1673 mL	20.8364 mL
10 mM	0.2084 mL	1.0418 mL	2.0836 mL	10.4182 mL
20 mM	0.1042 mL	0.5209 mL	1.0418 mL	5.2091 mL
50 mM	0.0417 mL	0.2084 mL	0.4167 mL	2.0836 mL
100 mM	0.0208 mL	0.1042 mL	0.2084 mL	1.0418 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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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