RO4987655
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 |
|---|---|---|
| 100mg | $1750 | Check With Us |
| 250mg | $2350 | Check With Us |
| 500mg | $3525 | Check With Us |
: Cat #: V3012 CAS #: 874101-00-5 Purity ≥ 98%
Description: RO4987655 (also known as CH-4987655) is a novel, orally bioavailable and specific small molecule inhibitor of MEK kinase with an IC50 of 5.2 nM for MEK1/MEK2.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
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- Quality Control Documentation
| Molecular Weight (MW) | 565.28 |
|---|---|
| Molecular Formula | C20H19F3IN3O5 |
| CAS No. | 874101-00-5 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: ≥ 40 mg/mLr |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| SMILES Code | O=C(NOCCO)C1=CC(CN2OCCCC2=O)=C(F)C(F)=C1NC3=CC=C(I)C=C3F |
| Synonyms | CH4987655; CH-4987655; CH 4987655; RO4987655; RO-4987655; RO 4987655 |
| Protocol | In Vitro | RO4987655 potently inhibits mitogen-activated protein kinase signaling pathway activation and tumor cell growth, with an in vitro IC50 of 5.2 nM for inhibition of MEK1/2. |
|---|---|---|
| In Vivo | Single-agent oral administration of RO4987655 (CH4987655) results in complete tumor regressions in xenograft models. RO4987655 is rapidly absorbed with a tmax of ~1 h. Exposures are dose proportional from 0.5 to 4 mg. The disposition is biphasic with a terminal t1/2 of ~25 hr. Intersubject variability is low, 9% to 23% for Cmax and 14% to 25% for area-under-the-curve (AUC). pERK inhibition is exposure dependent and is greater than 80% inhibition at higher doses. The pharmacokinetic-pharmacodynamic relationship is characterized by an inhibitory Emax model (Emax ~100%; IC50 40.6 ng/mL) using nonlinear mixed-effect modeling. |
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 | 1.7690 mL | 8.8452 mL | 17.6903 mL | 35.3807 mL |
| 5mM | 0.3538 mL | 1.7690 mL | 3.5381 mL | 7.0761 mL |
| 10mM | 0.1769 mL | 0.8845 mL | 1.7690 mL | 3.5381 mL |
| 20mM | 0.0885 mL | 0.4423 mL | 0.8845 mL | 1.7690 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:
Working concentration:
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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.