Discontinued Product

Selumetinib (Cat. No. 6815) has been withdrawn from sale for commercial reasons.
Description: Potent and selective MEK inhibitor; orally bioavailable
Chemical Name: 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
Purity: ≥98% (HPLC)
Citations (1)
Literature (1)
Pathways (1)

Biological Activity for Selumetinib

Selumetinib is a potent and selective MEK inhibitor (IC50 = 14 nM for MEK1, Kd = 530 nM for MEK2). Inhibits ERK1/2 phosphorylation (IC50 = 10 nM). Exhibits no activity at p38α, MKK6, EGFR, ErbB2 and ERK2. Suppresses several cell lines containing B-Raf and Ras mutations, but displays no effect on a normal fibroblast cell lines. Inhibits tumor growth in colorectal tumor xenograft model. Orally bioavailable.

Technical Data for Selumetinib

M. Wt 457.68
Formula C17H15BrClFN4O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 606143-52-6
PubChem ID 10127622
Smiles CN1C=NC2=C(C(NC3=C(C=C(C=C3)Br)Cl)=C(C(NOCCO)=O)C=C12)F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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Keywords: Selumetinib, Selumetinib supplier, Potent, selective, MEK, inhibitors, inhibits, ERK1/2, orally, bioavailable, active, in, vivo, 6815, Tocris Bioscience

1 Citation for Selumetinib

Citations are publications that use Tocris products. Selected citations for Selumetinib include:

Jonathan A et al (2023) Deep genomic analysis of malignant peripheral nerve sheath tumor cell lines challenges current malignant peripheral nerve sheath tumor diagnosis. iScience 26 106096 PMID: 36818284

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

MAPK Signaling Scientific Review

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.

Pathways for Selumetinib

MAPK Signaling Pathway

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.