VX-11e

"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

相关产品

SCH772984-GDC-0994-XMD8-92-TIC10-FR 180204-Tauroursodeoxycholate Sodium-Tomatidine-VRT752271-APS-2-79-Corynoxeine-Astragaloside IV-DEL-22379-XMD17-109-ERK5-IN-1-Mogrol-

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.