VX-11e (Synonyms: TCS Extracellular Signal-Related Kinase 11e, VX-11e) |
Catalog No.GC13115 |
A selective ERK inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 896720-20-0
Sample solution is provided at 25 µL, 10mM.
VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
VX-11e is active in the HT29 cell proliferation assay (IC50=48 nM)[1].
VX-11e is orally bioavailable in both rat and mice[1]. VX-11e (50 mg/kg, p.o.) results in robust inhibition of pRSK, and inhibits tumor growth in NSG mice bearing human melanoma RPDX tumors. VX-11e with BKM120 significantly improves tumor growth inhibition[2].
References:
[1]. Aronov, Alex M., et al. Structure-Guided Design of Potent and Selective Pyrimidylpyrrole Inhibitors of Extracellular Signal-Regulated Kinase (ERK) Using Conformational Control. Journal of Medicinal Chemistry (2009), 52(20), 6362-6368.
[2]. Krepler C, et al. Personalized Preclinical Trials in BRAF Inhibitor-Resistant Patient-Derived Xenograft Models Identify Second-Line Combination Therapies. Clin Cancer Res. 2016 Apr 1;22(7):1592-602.
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