All AbMole products are for research use only, cannot be used for human consumption.
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 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related MEK Products |
|---|
| AS703026
Pimasertib (AS-703026) is a novel selective MEK1/2 inhibitor, and induces pleiotropic anti-myeloma activity in vitro and in vivo. |
| AZD6244
AZD6244 (ARRY-142886, Selumetinib) is a potent MEK 1/2 inhibitor with GI50 values ranging from 14 to 50 nM. |
| AZD8330
AZD8330 (ARRY-424704) is a novel, selective, highly efficacious, uncompetitive MEK inhibitor with an IC50 of 7 nM. |
| CI-1040
CI-1040 (PD184352) is a targeted signal transduction inhibitor of MEK with a ki value of 300nM in vitro. |
| TAK-733
TAK-733 is a potent and selective MEK allosteric site inhibitor with IC50 of 3.2nM for the treatment of cancer. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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