Binimetinib ( Mektovi; ARRY438162; ARRY162; MEK162)
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 |
|---|---|---|
| 500mg | $270 | Check With Us |
| 1g | $470 | Check With Us |
| 5g | $1185 | Check With Us |
: Cat #: V0454 CAS #: 606143-89-9 Purity ≥ 98%
Description: Binimetinib (trade name: Mektovi; formerly ARRY-438162; ARRY-162; MEK-162) is a highly selective and orally bioavailable MEK1/2 (mitogen-activated protein kinase kinase) inhibitor with potential antineoplastic activity.
References: J Pheneger, et al. 2006, ACR Annual Scientific Meeting. Abst 794.
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- Related Biological Data
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| Molecular Weight (MW) | 441.23 |
|---|---|
| Molecular Formula | C17H15BrF2N4O3 |
| CAS No. | 606143-89-9 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 88 mg/mL (199.4 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 1% CMC+0.5% Tween-80: 30 mg/mL |
| SMILES Code | O=C(C1=C(NC2=CC=C(Br)C=C2F)C(F)=C3N=CN(C)C3=C1)NOCCO |
| Synonyms | MEK162; ARRY 162; ARRY438162; ARRY-162, ARRY-438162; MEK 162; MEK-162; ARRY162; ARRY-162; ARRY-438162; Binimetinib; Brand name: Mektovi |
| Protocol | In Vitro | In MCF7 cells, RSK3 or RSK4 expression decreases response to treatment with any of the PI3K inhibitors alone. However, the combination of PI3K inhibition with Binimetinib (MEK162) or BI-D1870 completely reverses the resistance of RSK-expressing cells. |
|---|---|---|
| In Vivo | Treatment with Binimetinib (ARRY-438162) reduces disease severity in a dose-related manner in both animal models. ARRY-438162 in the CIA model inhibits increases in ankle diameter by 27% and 50% at 1 and 3 mg/kg, while Ibuprofen has 46% inhibition. When combined with Ibuprofen, these same two doses result in 74% and 72% inhibition, respectively. Microscopic examination of the ankle joints show Binimetinib (ARRY-438162) significantly inhibits lesions (inflammation, cartilage damage, pannus formation and bone resorption) by 32% and 60% at 1 and 3 mg/kg, while treatment with Ibuprofen alone results in 17% inhibition, which is not significantly different from the controls. When these two doses of Binimetinib (ARRY-438162) are combined with ibuprofen, the result is 54% and 77% inhibition of joint destruction. In AIA, 3 and 10 mg/kg of Binimetinib (ARRY-438162) inhibit AIA ankle diameter 11% and 34%, while MTX has 33% inhibition. When combined with MTX, 3 and 10 mg/kg of Binimetinib (ARRY-438162) result in 55% and 71% inhibition. Microscopic examination of ankle joints for inflammation and bone resorption also shows improved efficacy versus either compound alone. |
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 | 2.2664 mL | 11.3320 mL | 22.6639 mL | 45.3278 mL |
| 5mM | 0.4533 mL | 2.2664 mL | 4.5328 mL | 9.0656 mL |
| 10mM | 0.2266 mL | 1.1332 mL | 2.2664 mL | 4.5328 mL |
| 20mM | 0.1133 mL | 0.5666 mL | 1.1332 mL | 2.2664 mL |
The molarity calculator equation
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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
+
%
+
%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.