UlixertinibUlixertinib
MedChemExpress (MCE)
HY-15816
869886-67-9
BVD-523
VRT752271
99.95%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
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 ERK2. Ulixertinib (BVD-523
VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.
Combined Ulixertinib (BVD-523
10, 20, 30 μM
48 hours) and VS-5584 treatment causes significant induction of cell death in human pancreatic cancer (HPAC) cells in PDAC cell lines BxPC-3, MIAPaCa-2, and CFPAC-1[3].
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].
ERK2 0.3 nM (IC50, at KM ATP (60 μM)) ERK1
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[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. [Content Brief]
[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. [Content Brief]
[3]. Changwen Ning, et al. Targeting ERK Enhances the Cytotoxic Effect of the Novel PI3K and mTOR Dual Inhibitor VS-5584 in Preclinical Models of Pancreatic Cancer. Oncotarget. 2017 Jul 4
8(27):44295-44311. [Content Brief]