Trametinib-13C,d3
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.
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- No. CAS: 2712126-59-3
- Fòrmula: C2513CH20D3FIN5O4
- Peso molecular:619.41
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
In Vitro
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[88].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Aplicación
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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No. CAS 2712126-59-3
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Unlabeled CAS 871700-17-3
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Peso molecular 619.41
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Fòrmula C2513CH20D3FIN5O4
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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
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Synonyms
GSK1120212-13C,d3; JTP-74057-13C,d3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Trametinib-13C,d3 Related Classifications
HY-10999S2 Related Classifications
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