RAF709
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1080 | Check With Us |
| 500mg | $1550 | Check With Us |
| 1g | $2325 | Check With Us |
: Cat #: V2920 CAS #: 1628838-42-5 Purity ≥ 98%
Description: RAF709 is a novel and potent inhibitor of the Raf kinase B/C isoforms (compound example 131 from patent WO2014151616A1) developed through a hypothesis-driven approach focusing on drug-like properties.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 542.55 |
|---|---|
| Molecular Formula | C28H29F3N4O4 |
| CAS No. | 1628838-42-5 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 100 mg/mLr |
| Water: <1 mg/mLr | |
| Ethanol: 100 mg/mL | |
| SMILES Code | O=C(NC1=CN=C(C)C(C2=CC(N3CCOCC3)=C(OC4CCOCC4)N=C2)=C1)C5=CC=CC(C(F)(F)F)=C5 |
| Synonyms | RAF-709; RAF709; RAF 709 |
| Protocol | In Vitro | RAF709 stabilizes BRAF-CRAF dimers with an EC50 of 0.8 μM. In cellular assays, the dose-response of pMEK and pERK are measured in Calu-6 cells with EC50=0.02 and 0.1 μM with minimal paradoxical activation and inhibition of proliferation with EC50=0.95 μM. |
|---|---|---|
| In Vivo | RAF709 proves to be soluble, kinase selective, and efficacious in a KRAS mutant xenograft model. RAF709 shows dose-proportional increases in plasma exposure and a corresponding dosedependent inhibition of pERK in Calu-6 tumors. Treatment with RAF709 results in dose-dependent antitumor activity with 10 mg/kg being subefficacious (%T/C=92%), 30 mg/kg results in measurable antitumor activity (%T/C=46%), and 200 mg/kg results in mean tumor regression of 92%, while the same high dose is not efficacious in the PC3, KRAS WT model. |
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 | 1.8431 mL | 9.2157 mL | 18.4315 mL | 36.8630 mL |
| 5mM | 0.3686 mL | 1.8431 mL | 3.6863 mL | 7.3726 mL |
| 10mM | 0.1843 mL | 0.9216 mL | 1.8431 mL | 3.6863 mL |
| 20mM | 0.0922 mL | 0.4608 mL | 0.9216 mL | 1.8431 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
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%ddH2O
Calculation Results:
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Method for preparing DMSO master liquid:
mg
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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.