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Trametinib-13C, d3

CAT: 0804-HY-10999S2Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-10999S2Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
Trametinib-13C, d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
CAS Number
2712126-59-3
Product Name Alternative
GSK1120212-13C, d3; JTP-74057-13C, d3
UNSPSC
12352005
Target
Apoptosis; Autophagy; Isotope-Labeled Compounds; MEK
Type
Isotope-Labeled Compounds
Related Pathways
Apoptosis; Autophagy; MAPK/ERK Pathway; Others
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Solubility
10 mM in DMSO
Smiles
CC(NC1=CC=CC(N(C(C(C(N2C3CC3)=O)=C(NC4=CC=C(I)C=C4F)N5C)=C([13C]([2H])([2H])[2H])C5=O)C2=O)=C1)=O
Molecular Formula
C25 13CH20D3FIN5O4
Molecular Weight
619.41
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-223.|[2]Abe H, et al. Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate) . ACS Med Chem Lett. 2011 Feb 28;2 (4) :320-4.|[3]Lai J, et al. Elimination of melanoma by sortase A-generated TCR-like antibody-drug conjugates (TL-ADCs) targeting intracellular melanoma antigen MART-1. Biomaterials. 2018 Sep;178:158-169.|[4]Liu H, et al. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple Negative Breast Cancer. Cancer Discov. 2018 Mar;8 (3) :354-369.|[5]Yamaguchi T, et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol, 2011, 39 (1), 23-31.|[6]Yamaguchi T, et al. Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with HWA486. Inflamm Res, 2012, 61 (5), 445-454.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

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