WX-554 is an orally available small molecule mitogen-activated protein kinase kinase (MAP2K, MAPK/ERK kinase, or MEK) inhibitor, with potential antineoplastic activity. MEK inhibitor WX-554 selectively binds to and inhibits the activity of MEK, thereby preventing the activation of MEK-dependent effector proteins including some transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK, a dual-specificity threonine/tyrosine kinase that plays a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway, is frequently upregulated in a variety of tumor cell types.
| Catalog Number | I009772 |
| Synonyms | ;NONE |
| Purity | ≥95% |
| Target | MEK inhibitor |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| Reference | </br>1:Enhanced anti-tumour activity of the combination of the novel MEK inhibitor WX-554 and the novel PI3K inhibitor WX-037. Haagensen EJ, Thomas HD, Schmalix WA, Payne AC, Kevorkian L, Allen RA, Bevan P, Maxwell RJ, Newell DR.Cancer Chemother Pharmacol. 2016 Dec;78(6):1269-1281. Epub 2016 Nov 11. PMID: 27837257 Free PMC Article</br>2:A phase I pharmacokinetic and pharmacodynamic study of the oral mitogen-activated protein kinase kinase (MEK) inhibitor, WX-554, in patients with advanced solid tumours. Jamieson D, Griffin MJ, Sludden J, Drew Y, Cresti N, Swales K, Merriman M, Allen R, Bevan P, Buerkle M, Mala C, Coyle V, Rodgers L, Dean E, Greystoke A, Banerji U, Wilson RH, Evans TR, Anthoney A, Ranson M, Boddy AV, Plummer R.Eur J Cancer. 2016 Nov;68:1-10. doi: 10.1016/j.ejca.2016.08.026. Epub 2016 Sep 28. PMID: 27693888 |
