[CAS NO. 1286739-19-2] FRAX597
PRODUCTS SPECIFICATIONS [1286739-19-2]
DESCRIPTION [1286739-19-2]
Overview
| MDL | MFCD25976723 |
|---|---|
| Molecular Weight | 558.10 |
| Molecular Formula | C29H28ClN7OS |
| SMILES | O=C1C(C2=CC=C(C3=CN=CS3)C=C2Cl)=CC4=CN=C(NC5=CC=C(N6CCN(C)CC6)C=C5)N=C4N1CC |
4 Publications Citing Use of MCE
Summary
IC50 & Target
|
PAK1 8 nM (IC 50 ) |
PAK2 13 nM (IC 50 ) |
PAK3 19 nM (IC 50 ) |
In Vitro
FRAX597 is determined to be a potent, ATP-competitive inhibitor of group I PAKs (PAK 1-3), with biochemical IC 50 values as follows: PAK1 IC 50 =8 nM, PAK2 IC 50 =13 nM, PAK3 IC 50 =19 nM. The IC 50 toward PAK4, a member of group II PAKs is >10 μM. At a concentration of 100 nM FRAX597 displays a significant (>80% inhibition) inhibitory capacity toward YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%). When measured using the Kinase Glo Assay in the presence of 20 nM protein and 1 μM ATP, FRAX597 displayed an IC 50 value of 48 nM against wild type PAK1, while IC 50 values against the V342F and V342Y PAK1 mutants are higher than 3 μM and 2 μM, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Analysis of the flux reading for the animals in the two cohorts demonstrates a significantly slower tumor growth rate in FRAX597-treated mice compared with control mice. After 14 days of treatment the animals are sacrificed and the tumors excised and weighed. FRAX597-treated cohort shows significantly lower average tumor weight compared with the control cohort (0.55 g versus 1.87 g, p=0.0001) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 14.29 mg/mL ( 25.60 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7918 mL | 8.9590 mL | 17.9179 mL |
| 5 mM | 0.3584 mL | 1.7918 mL | 3.5836 mL |
| 10 mM | 0.1792 mL | 0.8959 mL | 1.7918 mL |