VRT752271 |
| Catalog No.GC17031 |
VRT752271 (BVD-523; VRT752271) es un inhibidor covalente reversible, potente, activo por vÍa oral, altamente selectivo, competitivo con ATP de las quinasas ERK1/2, con una IC50 de <0,3 nM contra ERK2. VRT752271 (BVD-523; VRT752271) inhibe el ERK2 fosforilado (pERK) y la quinasa RSK corriente abajo (pRSK) en una lÍnea celular de melanoma A375.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 869886-67-9
Sample solution is provided at 25 µL, 10mM.
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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].
References:
[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.
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