Selumetinib is a non-ATP competitive inhibitor of MEK-1 (IC50 = 14 nM). This compound inactivates the phosphorylation of ERK1/2 (IC50 < 40 nM). Selumetinib has little effect on p38, c-Jun-NH2-kinase, or the MEK/ERK5 pathways.Potent, selective, non-ATP com
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ALLOSTERIC MODULATOR, INHIBITOR
Mechanism of action
Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3. A MEK-1 non-ATP competitive inhibitor.
Product Properties
ALogP
3.6
Associated Targets
CTNNBIP1Tbio Beta-catenin-interacting protein 1 0 Activities
1.Davies H, Bignell GR, Cox C, Stephens P, Edkins S, Clegg S, Teague J, Woffendin H, Garnett MJ, Bottomley W et al.. (2002) Mutations of the BRAF gene in human cancer.. Nature, 417 (6892):(949-54). [PMID:12068308]
2.Huynh H, Soo KC, Chow PK, Tran E. (2007) Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma.. Mol Cancer Ther, 6 (1):(138-46). [PMID:17237274]
3.Troiani T, Vecchione L, Martinelli E, Capasso A, Costantino S, Ciuffreda LP, Morgillo F, Vitagliano D, D'Aiuto E, De Palma R et al.. (2012) Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase A activation in human lung and colorectal cancer cells.. Br J Cancer, 106 (10):(1648-59). [PMID:22569000]
4.Dombi E, Baldwin A, Marcus LJ, Fisher MJ, Weiss B, Kim A, Whitcomb P, Martin S, Aschbacher-Smith LE, Rizvi TA et al.. (2016) Activity of Selumetinib in Neurofibromatosis Type 1-Related Plexiform Neurofibromas.. N Engl J Med, 375 (26):(2550-2560). [PMID:28029918]
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C2409113