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MEK&P38 MAPK

Binimetinib (MEK162) (606143-89-9)

MEK162(ARRY-438162; ARRY-162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM.Binimetinib, also known as MEK162 (ARRY-162), is an oral, highly selective MEK inhibitor.

Not Intended for Therapeutic Use. For research use only.

CAS: 606143-89-9 Category

Binimetinib (MEK162) (606143-89-9) Description:

Binimetinib, also known as MEK162 (ARRY-162), is an oral, highly selective MEK inhibitor. In preclinical studies, MEK162 showed significant antitumor activities in cell lines and animal models. MEK162 is the first targeted therapy to show activity in patients with NRAS -mutated melanoma and might offer a new option for a cancer with few effective treatments.

Binimetinib is an orally available inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2) with potential antineoplastic activity. Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. Inhibition of MEK1/2 prevents the activation of MEK1/2 dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling. This may eventually lead to an inhibition of tumor cell proliferation and an inhibition in production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor. MEK1/2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types.

Binimetinib (MEK162) (606143-89-9) Specifications:

Product Name Binimetinib (MEK-162)
Synonym MEK162; MEK-162; MEK 162; ARRY162; ARRY-162; ARRY 162; ARRY438162, Binimetinib
Chemical Name 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide.
Drug Class N/A
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 606143-89-9
Molecular Formula C17H15BrF2N4O3
Molecular Weight 441.22681
Monoisotopic Mass
440.03 g/mol

 

MDL number MFCD22124525
InChIKey ACWZRVQXLIRSDF-UHFFFAOYSA-N
InChi Code InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)
SMILES O=C(C1=C(NC2=CC=C(Br)C=C2F)C(F)=C3N=CN(C)C3=C1)NOCCO
Form solid powder
Color N/A
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application Binimetinib is an orally available inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2) with potential antineoplastic activity.

 


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RIDADR NONH for all modes of transport

References:

1: Hamidi H, Lu M, Chau K, Anderson L, Fejzo M, Ginther C, Linnartz R, Zubel A, Slamon DJ, Finn RS. KRAS mutational subtype and copy number predict in vitro response of human pancreatic cancer cell lines to MEK inhibition. Br J Cancer. 2014 Aug 28. doi: 10.1038/bjc.2014.475. [Epub ahead of print] PubMed PMID: 25167228.

2: Rebecca VW, Alicea GM, Paraiso KH, Lawrence H, Gibney GT, Smalley KS. Vertical inhibition of the MAPK pathway enhances therapeutic responses in NRAS-mutant melanoma. Pigment Cell Melanoma Res. 2014 Aug 11. doi: 10.1111/pcmr.12303. [Epub ahead of print] PubMed PMID: 25130256.

3: Urner-Bloch U, Urner M, Stieger P, Galliker N, Winterton N, Zubel A, Moutouh-de Parseval L, Dummer R, Goldinger SM. Transient MEK inhibitor-associated retinopathy in metastatic melanoma. Ann Oncol. 2014 Jul;25(7):1437-41. doi: 10.1093/annonc/mdu169. Epub 2014 May 26. PubMed PMID: 24864047.

4: Küsters-Vandevelde HV, Willemsen AE, Groenen PJ, Küsters B, Lammens M, Wesseling P, Djafarihamedani M, Rijntjes J, Delye H, Willemsen MA, van Herpen CM, Blokx WA. Experimental treatment of NRAS-mutated neurocutaneous melanocytosis with MEK162, a MEK-inhibitor. Acta Neuropathol Commun. 2014 Apr 8;2(1):41. doi: 10.1186/2051-5960-2-41. PubMed PMID: 24713450; PubMed Central PMCID: PMC4023633.

5: Thumar J, Shahbazian D, Aziz SA, Jilaveanu LB, Kluger HM. MEK targeting in N-RAS mutated metastatic melanoma. Mol Cancer. 2014 Mar 4;13:45. doi: 10.1186/1476-4598-13-45. PubMed PMID: 24588908; PubMed Central PMCID: PMC3945937.

1 review for Binimetinib (MEK162) (606143-89-9)

  1. Cofttek

    Never had such good experience before,The Binimetinib (MEK162) (606143-89-9) is high purity,also customer service is pretty nice !gotta try!!

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