Catalog No.S7271

For research use only.

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.

FRAX597 Chemical Structure

CAS No. 1286739-19-2

Selleck's FRAX597 has been cited by 24 publications

Purity & Quality Control

Choose Selective PAK Inhibitors

Biological Activity

Description 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.
PAK1 [1]
(Cell-free assay)
PAK2 [1]
(Cell-free assay)
PAK3 [1]
(Cell-free assay)
8 nM 13 nM 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%). FRAX597 treatment dramatically impairs the proliferation of Nf2-null SC4 Schwann cells (SC4 cells). FRAX597 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] FRAX597 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]

Methods Test Index PMID
Western blot p-PAK1 / PAK1 23960073
Growth inhibition assay Cell proliferation ; Migration and invasion ; Cell viability 26774265
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, FRAX597 (90 mg/kg/day, p.o.) significantly suppresses tumor growth.[2] In KrasG12D mice, treatment with FRAX597 (90 mg/kg/day, p.o.) causes tumor regression and loss of Erk and Akt activity.[3]

Protocol (from reference)

Kinase Assay:[1]
  • Determination of Enzyme IC50 Values:

    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.

Cell Research:[1]
  • Cell lines: SC4 cells
  • Concentrations: 1 μM
  • Incubation Time: 4 day
  • Method: 30,000 cells/well are plated in 12-well dishes in triplicate. Cell growth media with or without FRAX597 is replaced daily. At indicated time points, cells from individual wells are trypsinized and counted using a Coulter counter.
Animal Research:[2]
  • Animal Models: SCID mice with orthotopic meningioma model
  • Dosages: 90 mg/kg/day
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 558.10


CAS No. 1286739-19-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy FRAX597|FRAX597 ic50|FRAX597 price|FRAX597 cost|FRAX597 solubility dmso|FRAX597 purchase|FRAX597 manufacturer|FRAX597 research buy|FRAX597 order|FRAX597 mouse|FRAX597 chemical structure|FRAX597 mw|FRAX597 molecular weight|FRAX597 datasheet|FRAX597 supplier|FRAX597 in vitro|FRAX597 cell line|FRAX597 concentration|FRAX597 nmr|FRAX597 in vivo|FRAX597 clinical trial|FRAX597 inhibitor|FRAX597 Cytoskeletal Signaling inhibitor