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Binimetinib

Catalog No. T2508   CAS 606143-89-9
Synonyms: ARRY-438162, ARRY-162, MEK162

Binimetinib (ARRY-162) (MEK162, ARRY-162, ARRY-438162) is an orally available inhibitor of MEK1/2 (IC50: 12 nM) in a cell-free assay.

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Binimetinib Chemical Structure
Binimetinib, CAS 606143-89-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 35.00
10 mg In stock $ 57.00
25 mg In stock $ 68.00
50 mg In stock $ 80.00
100 mg In stock $ 97.00
200 mg In stock $ 155.00
1 mL * 10 mM (in DMSO) In stock $ 63.00
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Purity: 100%
Purity: 99%
Purity: 98.03%
Purity: 98.03%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Binimetinib (ARRY-162) (MEK162, ARRY-162, ARRY-438162) is an orally available inhibitor of MEK1/2 (IC50: 12 nM) in a cell-free assay.
Targets&IC50 MEK:12 nM
Cell Research MEK162 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. MCF7 cells infected as indicated are seeded in 12-well plates (2×104). After 24 hours, cells are treated with BEZ235 (100 or 200 nM), BKM120 (0.75 or 1 μM), GDC-0941 (1 μM), or MK2206 (2 μM) alone or in combination with MEK162 (1 μM), BI-D1870 (10 μM), or AZD6244 (1 μM), as indicated in text. Cell numbers are quantified by fixing cells with 4% glutaraldehyde or methanol, washing the cells twice in Water, and staining the cells with 0.1% crystal violet. The dye is subsequently extracted with 10% acetic acid, and its absorbance is determined (570 nm). Growth curves are performed in triplicate. Viability assays with CellTiter-Glo are performed by plating 2,000 cells in 96-well plates, adding the drug at 24 hours, and assaying 4 to 5 days after drug addition. Cell-cycle and hypodiploid apoptotic cells are quantified by flow cytometry. Briefly, cells are washed with PBS, fixed in cold 70% ethanol, and then stained with propidium iodide while being treated with RNase. Quantitative analysis of sub-G1 cells is carried out in a FACScalibur cytometer using Cell Quest software[2].
Synonyms ARRY-438162, ARRY-162, MEK162
Molecular Weight 441.23
Formula C17H15BrF2N4O3
CAS No. 606143-89-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 82 mg/mL (185.8 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. J Pheneger, et al. 2006, ACR Annual Scientific Meeting. Abst 794. 2. D Wright, et al. 2009, Arraybiopharma. Abstract FRI0063. 3. SS Bhagwat, et al. Annu Rep Med Chem, 2007, 42, 265–278. 4. Serra V, et al. J Clin Invest, 2013, 123(6), 2551-2563. 6. Cheng H, et al. PIK3CA(H1047R)- and Her2-initiated mammary tumors escape PI3K dependency by compensatory activation of MEK-ERK signaling. Oncogene. 2016 Jun 9;35(23):2961-70. 7. Seip K, et al. Fibroblast-induced switching to the mesenchymal-like phenotype and PI3K/mTOR signaling protects melanoma cells from BRAF inhibitors. Oncotarget. 2016 Apr 12;7(15):19997-20015.

TargetMolCitations

1. Fan K, Ni X, Shen S, et al. Acetylation stabilizes stathmin1 and promotes its activity contributing to gallbladder cancer metastasis. Cell Death Discovery. 2022, 8(1): 1-13

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Apoptosis Compound Library MAPK Inhibitor Library Fluorochemical Library Drug Repurposing Compound Library Bioactive Compounds Library Max

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Keywords

Binimetinib 606143-89-9 Autophagy MAPK MEK Inhibitor MEK-162 Mitogen-activated protein kinase kinase MEK 162 ARRY 162 ARRY162 ARRY438162 MAPKK MAP2K ARRY 438162 ARRY-438162 inhibit ARRY-162 MEK162 inhibitor

 

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