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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].

Product Specifications

CAS Number

[871700-17-3]

Product Name Alternative

GSK1120212; JTP-74057

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; MEK

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Trametinib.html

Purity

99.93

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC(NC1=CC=CC(N(C2=O)C(C(C(N2C3CC3)=O)=C(N4C)NC5=CC=C(C=C5F)I)=C(C4=O)C)=C1)=O

Molecular Formula

C26H23FIN5O4

Molecular Weight

615.39

Precautions

H302, H315, H319, H335

References & Citations

[1]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.|[2]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.|[3]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.|[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]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

Reference compound1

Clinical Information

Launched

Isoform

MEK1; MEK2

Citation 01

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