FRAX597 [1286739-19-2]
Referência NB-64-30586-5mg
Tamanho : 5mg
Marca : Neo Biotech
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FRAX597
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Catalog No. T6014 Copy Product Info
Purity: 99.85%
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).
Cas No. 1286739-19-2
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.85%
Color:White to Yellow
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Product Information
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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, PAK2:13 nM, PAK1:8 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 |
| Smiles | CCn1c2nc(Nc3ccc(cc3)N3CCN(C)CC3)ncc2cc(-c2ccc(cc2Cl)-c2cncs2)c1=O |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 13.06 mg/mL (23.4 mM), Sonication is recommended.  | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: < 1.31 mg/mL (2.35 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1.33 mg/mL (2.38 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||