| Name | FRAX597 |
| 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). |
| 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) |
| 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. |
| 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%). |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 13.06 mg/mL (23.4 mM), Sonication is recommended.
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| Keywords | PAK3 | PAK2 | PAK1 | PAK | p21 activated kinases | Inhibitor | inhibit | FRAX-597 | FRAX597 | FRAX 597 |
| Inhibitors Related | Fingolimod hydrochloride | ZINC194100678 | P505-15 Acetate | PIR 3.5 | PRT062607 hydrochloride | PF-3758309 hydrochloride | G-5555 | FRAX1036 | AZ13705339 | GNE 2861 | 5-Aminosalicylic Acid | AZA197 |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | Multi-Target Compound Library | Post-Translational Modification Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library |
United States
