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Trametinib-d4

CAT: 0804-HY-10999S-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-10999S-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
Trametinib-d4 is the 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].
UNSPSC
12352005
Target
Apoptosis; Autophagy; MEK
Type
Isotope-Labeled Compounds
Related Pathways
Apoptosis; Autophagy; MAPK/ERK Pathway
Field of Research
Cancer
Purity
99.87
Solubility
DMSO : 50 mg/mL (ultrasonic)
Smiles
CC(NC1=C(C([2H])=C(C(N(C(C(C(N2C3CC3)=O)=C(NC4=CC=C(I)C=C4F)N5C)=C(C)C5=O)C2=O)=C1[2H])[2H])[2H])=O
Molecular Formula
C26H19D4FIN5O4
Molecular Weight
619.42
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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.|[3]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.|[4]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.|[5]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.|[6]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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

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