FRAX597
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $1290 | Check With Us |
| 500mg | $1950 | Check With Us |
| 1g | $2975 | Check With Us |
: Cat #: V1595 CAS #: 1286739-19-2 Purity ≥ 99%
Description: FRAX597 (FRAX-597; FRAX 597) is a novel, potent and ATP-competitive inhibitor of group I PAKs (p21-activated Kinases) with potential anticancer activity.
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| Molecular Weight (MW) | 558.10 |
|---|---|
| Molecular Formula | C29H28ClN7OS |
| CAS No. | 1286739-19-2 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 14 mg/mL (25.1 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Synonyms | FRAX597; FRAX-597; FRAX 597 |
| Protocol | In Vitro | FRAX597 is determined to be a potent, ATP-competitive inhibitor of group I PAKs (PAK 1-3), with biochemical IC50 values as follows: PAK1 IC50=8 nM, PAK2 IC50=13 nM, PAK3 IC50=19 nM. The IC50 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 IC50 value of 48 nM against wild type PAK1, while IC50 values against the V342F and V342Y PAK1 mutants are higher than 3 μM and 2 μM, respectively |
|---|---|---|
| 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) |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.7918 mL | 8.9590 mL | 17.9179 mL | 35.8359 mL |
| 5mM | 0.3584 mL | 1.7918 mL | 3.5836 mL | 7.1672 mL |
| 10mM | 0.1792 mL | 0.8959 mL | 1.7918 mL | 3.5836 mL |
| 20mM | 0.0896 mL | 0.4479 mL | 0.8959 mL | 1.7918 mL |
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The dilution calculator equation
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Step One: Enter information below
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Average weight of animals g
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Step Two: Enter the in vivo formulation
%DMSO
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%
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%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.