"目录号: HY-14178
MAPK/ERK PathwayStem Cell/Wnt-
VX-11e 是一种高效的，具有选择性的，可口服的ERK抑制剂，Ki值 < 2 nM。
ERK
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生物活性
Description
VX-11e is a potent, selective, and orally bioavailable inhibitor ofERKwithKi< 2 nM.
In Vitro
VX-11e?is active in the HT29 cell proliferation assay (IC50=48 nM)[1].
In Vivo
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.