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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).
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).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $34 | In Stock | |
| 2 mg | $48 | In Stock | |
| 5 mg | $80 | In Stock | |
| 10 mg | $139 | In Stock | |
| 25 mg | $252 | In Stock | |
| 50 mg | $417 | In Stock | |
| 100 mg | $619 | In Stock | |
| 500 mg | $1,330 | In Stock |
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Purity:99.85%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 | PAK3:19 nM, PAK1:8 nM, PAK2:13 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 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO: 1 mg/ml, Sonication is recommended.  |
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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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