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FRAX597 PAK inhibitor

Name: FRAX597
Brand: Selleck Chemicals
SKU: S7271
Availability: InStock
Rating: 5 (35 reviews)

Cat.No.S7271

FRAX597 is a potent, ATP-competitive inhibitor of group I PAKs with IC50 of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively.

Chemical Structure

Molecular Weight: 558.10

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.96%

99.96

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Chemical Information, Storage & Stability

Molecular Weight	558.10	Formula	C₂₉H₂₈ClN₇OS	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1286739-19-2	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)C4=CN=CS4)Cl)NC5=CC=C(C=C5)N6CCN(CC6)C

Solubility

In vitro
Batch:

DMSO : 5 mg/mL (8.95 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.45mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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.

Mechanism of Action

Targets/IC₅₀/Ki	PAK1 ^[1] (Cell-free assay) 8 nM PAK2 ^[1] (Cell-free assay) 13 nM PAK3 ^[1] (Cell-free assay) 19 nM
In vitro	FRAX597 (100 n M) displays a significant inhibitory capacity toward YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%), while displays minimal inhibitory activity towards the group II PAKs: PAK4 (0%), PAK6 (23%), and PAK7 (8%). This compound treatment dramatically impairs the proliferation of Nf2-null SC4 Schwann cells (SC4 cells). It displays an IC50 value of 48 nM against wild type PAK1, while IC 50 values against the V342F and V342Y PAK1 mutants are higher than 3μM and 2 μM, respectively.^[1] This chemical inhibits the proliferation and motility of both benign (Ben-Men1, 3μM) and malignant (KT21-MG1, 0.4 μM) meningiomas cells after treating of 72 h.^[2]
Kinase Assay	Determination of Enzyme IC50 Values
Kinase Assay	IC50 values are determined using a 10 concentration point, non-radioactive, functional assay that employs a fluorescence-based, coupled-enzyme format, according to the manufacturer’s protocol (Z’-LYTE^@biochemical assay). Kinase selectivity is determined using both the Z’-LYTE^@ and Adapta^@ kinase assay format.
In vivo	In NOD/SCID mice which bearing Nf2^-/-SC4 Schwann cells, FRAX597 (100 mg/kg/day, p.o.) causes more significant tumor growth inhibition cpmpared with control mice.^[1] In SCID mice with orthotopic meningioma, this compound (90 mg/kg/day, p.o.) significantly suppresses tumor growth.^[2] In Kras^G12D mice, treatment with this chemical (90 mg/kg/day, p.o.) causes tumor regression and loss of Erk and Akt activity.^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/23960073/ [2] https://pubmed.ncbi.nlm.nih.gov/25596744/ [3] https://pubmed.ncbi.nlm.nih.gov/22983922/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-PAK1 / PAK1		23960073
Growth inhibition assay	Cell proliferation Migration and invasion Cell viability		26774265

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Handling Instructions

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