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VRT752271
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。
VRT752271图片
CAS NO:869886-67-9
规格:98%
分子量:433.33
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
ERK1/ERK2 inhibitor
CAS:869886-67-9
分子式:C21H22Cl2N4O2
分子量:433.33
纯度:98%
存储:Store at -20°C

Background:

Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of<0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line[1][2].


In the pharmacokinetic study, the sensitivity and specificity of the assay are found to be sufficient for accurately characterizing the plasma pharmacokinetics of Ulixertinib (VRT752271) in Balb/C mice[2].


参考文献:
[1]. Ward RA, et al. Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. J Med Chem. 2015 Jun 11;58(11):4790-801.
[2]. Kumar R, et al. Determination of ulixertinib in mice plasma by LC-MS/MS and its application to a pharmacokinetic study in mice. J Pharm Biomed Anal. 2016 Jun 5;125:140-4.