Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 34.00 | |
2 mg | In stock | $ 48.00 | |
5 mg | In stock | $ 80.00 | |
10 mg | In stock | $ 139.00 | |
25 mg | In stock | $ 252.00 | |
50 mg | In stock | $ 417.00 | |
100 mg | In stock | $ 619.00 | |
500 mg | In stock | $ 1,330.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 98.00 |
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). |
Targets&IC50 | PAK1:8 nM, PAK2:13 nM, PAK3:19 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) |
Molecular Weight | 558.1 |
Formula | C29H28ClN7OS |
CAS No. | 1286739-19-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 11.2 mg/mL (20 mM)
You can also refer to dose conversion for different animals. More
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FRAX597 1286739-19-2 Cytoskeletal Signaling PAK p21 activated kinases FRAX 597 Inhibitor inhibit FRAX-597 inhibitor