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FRAX597

FRAX597
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Purity:99.94%
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FRAX597

Catalog No. T6014Cas No. 1286739-19-2
FRAX597 is an effective, ATP-competitive inhibitor of group I PAKs, and for PAK1(IC50=8 nM), PAK2(IC50=13 nM), and PAK3 (IC50=19 nM).
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Pack SizePriceAvailabilityQuantity
1 mg$34In Stock
2 mg$48In Stock
5 mg$80In Stock
10 mg$139In Stock
25 mg$252In Stock
50 mg$417In Stock
100 mg$619In Stock
500 mg$1,330In Stock
1 mL x 10 mM (in DMSO)$98In Stock
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Product Introduction

Bioactivity
Description
FRAX597 is an effective, ATP-competitive inhibitor of group I PAKs, and for PAK1(IC50=8 nM), PAK2(IC50=13 nM), and PAK3 (IC50=19 nM).
In vitro
In NOD/SCID mice loaded with Nf2-/-SC4 Schwann cells, daily oral administration of FRAX597 (100 mg/kg) significantly inhibits tumor growth. Similarly, in SCID mice with intrinsic meningiomas, daily oral intake of FRAX597 (90 mg/kg) markedly suppresses tumor growth. Additionally, in KrasG12D mice, daily treatment with FRAX597 (90 mg/kg) leads to tumor regression and a decrease in Erk and Akt activity.
In vivo
FRAX597 exhibits potent inhibition against wild-type PAK1 (IC50=48 nM), whereas it shows significantly reduced efficacy against the V342F PAK1 mutation (IC50 > 3 μM) and the V342Y PAK1 mutation (IC50 > 2 μM). At a concentration of 100 nM, FRAX597 demonstrates substantial inhibitory effects on YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%).
Kinase Assay
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
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.(Only for Reference)
Chemical Properties
Molecular Weight558.1
FormulaC29H28ClN7OS
Cas No.1286739-19-2
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 11.2 mg/mL (20 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7918 mL8.9590 mL17.9179 mL89.5897 mL
5 mM0.3584 mL1.7918 mL3.5836 mL17.9179 mL
10 mM0.1792 mL0.8959 mL1.7918 mL8.9590 mL

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