Ro 5126766
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 | $1100 | Check With Us |
| 250mg | $1800 | Check With Us |
| 500mg | $2700 | Check With Us |
: Cat #: V3658 CAS #: 946128-88-7 Purity ≥ 98%
Description: Ro 5126766 (also known as Ro-5126766; CH5126766) is a novel, potent, first-in-class dual inhibitor of MEK/RAF mitogen-activated protein kinases (MAPKs) with anticancer activity.
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| Molecular Weight (MW) | 471.46 |
|---|---|
| Molecular Formula | C21H18FN5O5S |
| CAS No. | 946128-88-7 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | O=C1C(CC2=C(F)C(NS(=O)(NC)=O)=NC=C2)=C(C)C3=CC=C(OC4=NC=CC=N4)C=C3O1 |
| Synonyms | Avutometinib; RO5126766; RO 5126766; RO5126766; CH5126766; CH5126766; CH 5126766 |
| Protocol | In Vitro | Avutometinib (Ro 5126766) is an allosteric inhibitor that binds directly to MEK and prevents its phosphorylation by RAF through the formation of a stable RAF-MEK complex. Ro 5126766 inhibits both the phosphorylation of MEK by RAF and the activation of ERK by MEK. In cell-free MEK and RAF kinase assays, Avutometinib effectively inhibits activation of ERK2 by MEK1 with an IC50 of 160 nM (SD=±0.043) and inhibits the phosphorylation of MEK1 protein by BRAF (IC50=190 nM, SD=±0.003), BRAFV600E (IC50=8.2 nM, SD=±0.0015), and CRAF (IC50=56 nM, SD=±0.016). Avutometinib effectively inhibits both MEK and ERK phosphorylation in a panel of human tumor cell lines including KRAS/HRAS and BRAF mutant cell lines and KRAS/HRAS and BRAF wild-type cells. |
|---|---|---|
| In Vivo | In KRAS-mutant xenograft models, Avutometinib (Ro 5126766) inhibits growth and causes tumor regressions more effectively than another allosteric MEK inhibitor, PD0325901. Preclinical data from a series of human tumor mouse xenograft models indicates an ED50 for Ro 5126766 of 0.03 to 0.23 mg/kg and an ED90 of 0.15 to 1.56 mg/kg. These effective doses are associated with target trough concentrations of 17 to 133 ng/L and 87 to 901 ng/mL, respectively. . |
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 | 2.1211 mL | 10.6054 mL | 21.2107 mL | 42.4214 mL |
| 5mM | 0.4242 mL | 2.1211 mL | 4.2421 mL | 8.4843 mL |
| 10mM | 0.2121 mL | 1.0605 mL | 2.1211 mL | 4.2421 mL |
| 20mM | 0.1061 mL | 0.5303 mL | 1.0605 mL | 2.1211 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Volume
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Molecular Weight*
The dilution calculator equation
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Volume(start)
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,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.