Name: FRAX486
Brand: Selleck Chemicals
SKU: S7807
Availability: InStock
Rating: 5 (10 reviews)

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Quality Control

Batch: Purity: 99.89%

99.89

Related Targets	Akt Wnt/beta-catenin HSP PKC ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Other PAK Products	IPA-3 FRAX597 PF-3758309 FRAX1036 NVS-PAK1-1 LCH-7749944 Hydrastine PAK1 Antibody [P10N18] G-5555 GNE 2861

Solubility

In vitro
Batch:

DMSO : 15 mg/mL (29.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.97mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.97mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	513.39	Formula	C₂₅H₂₃Cl₂FN₆O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1232030-35-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=C(C=C3)Cl)Cl)NC4=CC(=C(C=C4)N5CCNCC5)F

Mechanism of Action

Targets/IC₅₀/Ki	PAK1 (Cell-free assay) 14 nM PAK2 (Cell-free assay) 33 nM PAK3 (Cell-free assay) 39 nM PAK4 (Cell-free assay) 575 nM
In vitro	In WPMY-1 cells, FRAX486 induces concentration-dependent (1-10 μM) degeneration of actin filaments. This was paralleled by attenuation of proliferation rate, being observed from 1 to 10 μM of this compound. Cytotoxicity of this chemical in WPMY-1 cells is time- and concentration-dependent. In WPMY-1 cells, effects of this compound on actin organization, survival, and proliferation occurred already at concentrations of 1-5 μM. In these concentrations, full inhibition of PAK1-3 may be expected, while PAK4 may be inhibited only partially.
In vivo	FRAX486 crosses the blood-brain barrier and that therapeutically useful concentrations of this compound are in the brain as early as 1 h and remain as long as 24 h after administration, with the maximum concentration in the target tissue at 8 h. Daily dosing results in steady-state levels of this chemical in the brain. It specifically rescues the Fmr1 KO abnormality in which the spine phenotype is present in apical neurons and not simply decreasing spine density irrespective of genotype or existence of a phenotype. Also, this compound reduces hyperactivity and stereotypical movements, both of which are phenotypes that characterize the mouse model of Fragile X syndrome.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24706880/ [2] https://pubmed.ncbi.nlm.nih.gov/27071060/ [3] https://pubmed.ncbi.nlm.nih.gov/23509247/

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FRAX486 PAK inhibitor

Chemical Structure

Molecular Weight: 513.39