Binimetinib-d3
Binimetinib-d3 (MEK162-d3) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
For research use only. We do not sell to patients.
- CAS No.: 2890696-59-8
- Formula: C17H12D3BrF2N4O3
- Molecular Weight:444.25
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All MEK Isoforms
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Biological Activity
Description
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 2890696-59-8
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Unlabeled CAS 606143-89-9
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Molecular Weight 444.25
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Formula C17H12D3BrF2N4O3
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SMILES
O=C(C1=C(NC2=CC=C(Br)C=C2F)C(F)=C3C(N(C([2H])([2H])[2H])C=N3)=C1)NOCCO
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Synonyms
MEK162-d3; ARRY-162-d3; ARRY-438162-d3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[2]. J Pheneger, et al. 2006, ACR Annual Scientific Meeting. Abst 794.
[3]. Kiessling MK, et al. Mutant HRAS as novel target for MEK and mTOR inhibitors. Oncotarget. 2015 Dec 8;6(39):42183-96. [Content Brief]
[4]. 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. [Content Brief]
[5]. Serra V, et al. RSK3/4 mediate resistance to PI3K pathway inhibitors in breast cancer. J Clin Invest, 2013, 123(6), 2551-2563. [Content Brief]
[6]. 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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)