Binimetinib-d4
Binimetinib-d4 (MEK162-d4) 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.: 2890696-60-1
- Formula: C17H11D4BrF2N4O3
- Molecular Weight:445.25
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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
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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. 2890696-60-1
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Unlabeled Cas 606143-89-9
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Molecular Weight 445.25
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Formula C17H11D4BrF2N4O3
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SMILES
FC1=C(NC2=C(F)C(N=CN3C)=C3C=C2C(NOC([2H])([2H])C([2H])([2H])O)=O)C=CC(Br)=C1
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Synonyms
MEK162-d4; ARRY-162-d4; ARRY-438162-d4
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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.
Purity & Documentation
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
[2]. 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]
[3]. 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]
[4]. Kiessling MK, et al. Mutant HRAS as novel target for MEK and mTOR inhibitors. Oncotarget. 2015 Dec 8;6(39):42183-96. [Content Brief]
[5]. J Pheneger, et al. 2006, ACR Annual Scientific Meeting. Abst 794.
[6]. 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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)