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.

Product Specifications

CAS Number

[2890696-60-1]

Product Name Alternative

MEK162-d4; ARRY-162-d4; ARRY-438162-d4

UNSPSC

12352005

Target

Autophagy; Isotope-Labeled Compounds; MEK

Related Pathways

Autophagy; MAPK/ERK Pathway; Others

Applications

COVID-19-immunoregulation

Field of Research

Cancer

Smiles

FC1=C(NC2=C(F)C(N=CN3C)=C3C=C2C(NOC([2H])([2H])C([2H])([2H])O)=O)C=CC(Br)=C1

Molecular Formula

C17H11D4BrF2N4O3

Molecular Weight

445.25

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[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.|[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.|[4]Kiessling MK, et al. Mutant HRAS as novel target for MEK and mTOR inhibitors. Oncotarget. 2015 Dec 8;6 (39) :42183-96.|[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.