FRAX597

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 23 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.
Targets
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]

Assay
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
Formula

C29H28ClN7OS

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

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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

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