Binimetinib-d3

• Description:

  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[1].

• Product Name Alternative:

  MEK162-d3; ARRY-162-d3; ARRY-438162-d3

• UNSPSC:

  12352005

• Target:

  Autophagy; Isotope-Labeled Compounds; MEK

• Type:

  Isotope-Labeled Compounds

• Related Pathways:

  Autophagy; MAPK/ERK Pathway; Others

• Field of Research:

  Cancer

• Smiles:

  O=C(C1=C(NC2=CC=C(Br)C=C2F)C(F)=C3C(N(C([2H])([2H])[2H])C=N3)=C1)NOCCO

• Molecular Formula:

  C17H12D3BrF2N4O3

• Molecular Weight:

  444.25

• References & Citations:

  [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.|[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.|[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.|[5]Serra V, et al. RSK3/4 mediate resistance to PI3K pathway inhibitors in breast cancer. J Clin Invest, 2013, 123 (6), 2551-2563.|[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.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Isotope-Labeled Compounds

• Clinical Information:

  No Development Reported

• CAS Number:

  [2890696-59-8]