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VX-11e
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VX-11e图片
CAS NO:896720-20-0
规格:98%
分子量:500.35
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
ERK inhibitor
CAS:896720-20-0
分子式:C24H20Cl2FN5O2
分子量:500.35
纯度:98%
存储:Store at -20°C

Background:

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].


参考文献:
[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.