ARRY-162 (Binimetinib; MEK162) is a selective, potent inhibitor of MEK and cellular pERK with IC50 of 12 nM and 11 nM, respectively. ARRY-162 (MEK-162) shows ex vivo inhibition of cytokine production such as IL-1, TNF and IL-6 in clinical trials. MEK signaling pathway acts as a central axis in the proliferation of different tumors including melanoma, non-small cell lung, head/neck and pancreatic cancers. And MEK inhibition is an important therapeutic strategy in treating cancer either alone or in combination with other agents. ARRY-162 has the potential to treat a range of malignant diseases.
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Cell Death Dis. 2014 Mar 20;5:e1134.
Overcoming inherent resistance to histone deacetylase inhibitors in multiple myeloma cells by targeting pathways integral to the actin cytoskeleton.
ARRY-162 (Binimetinib) purchased from AbMole
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Source | Cell Death and Disease (2014) 5, e1134. Figure 5. ARRY-162 were obtained from AbMole BioScience, HongKong, China, |
| Method | Flow cytometric enumeration of propidium iodide staining | |
| Cell Lines | U266, OPM2, RPMI8226, OCIMY1 | |
| Concentrations | 1µM | |
| Incubation Time | 72 hours | |
| Results | It was clear that LBH589 was found to be synergistic with MAPK and FAK inhibitors in all HMCL. |
| Cell Experiment | |
|---|---|
| Cell lines | A549 and H460 human lung cancer cell lines |
| Preparation method | Cells were collected and seeded in 96-well plates at a density of 5×103 cells/well. Human lung cancer A549 cells or H460 cells were untreated or treated with indicated concentration of perifosine (0.3–10 μM), in the presence or absence of MEK-162 (1 μM); for 24 or 72 h, cell growth was tested by MTT assay. |
| Concentrations | 1μM |
| Incubation time | 24 or 72 h |
| Animal Experiment | |
|---|---|
| Animal models | A549 lung cancer xenograft |
| Formulation | Formulated in 30% Captisol |
| Dosages | 2.5 mg/kg, once daily |
| Administration | lavage |
| Molecular Weight | 441.23 |
| Formula | C17H15BrF2N4O3 |
| CAS Number | 606143-89-9 |
| Solubility (25°C) | DMSO 65 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related MEK Products |
|---|
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Glycinexylidide (GX) is the active metabolite of Lidocaine. |
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Xantocillin (Xanthocillin X) is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway. |
| MEK-IN-6 hydrate
MEK-IN-6 hydrate is a MEK inhibitor. |
| MS934
MS934 is a novel improved VHL-recruiting MEK 1/2 degrader. |
| Nedometinib
Nedometinib is a tyrosine kinase inhibitor targeting to MEK1. |
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