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ARRY-162

Cat. No. M1744
ARRY-162 Structure
Synonym:

MEK-162, ARRY-438162

Size Price Availability Quantity
10mg USD 70 In stock
50mg USD 160 In stock
100mg USD 240 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

ARRY-162 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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 441.23
Formula C17H15BrF2N4O3
CAS Number 606143-89-9
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
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.
Rating
Product Citations
References

Combination treatment with perifosine and MEK-162 demonstrates synergism against lung cancer cells in vitro and in vivo
Jianli Zhang,et,al. Tumor Biol. 2015;36:5699–5706.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ARRY-162, MEK-162, ARRY-438162 supplier, MEK, inhibitors

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