Ulixertinib hydrochloride (BVD-523 hydrochloride) 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 hydrochloride is effective in inhibiting phosphorylated ERK2 (pERK) and the downstream kinase RSK (pRSK) in A375 melanoma cells[1].[2].
Ulixertinib HCl 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MRC5 cells
20 µM
30 minutes
Inhibition of ERK1/2 activity, blocking lactate-induced DRP1S616 phosphorylation
J Transl Med. 2024 May 21;22(1):479.
BT40 cells
62.7 nM
72 hours
Ulixertinib reduced metabolic activity in BT40 cells at clinically achievable concentrations, with an IC50 of 62.7 nM.
Neuro Oncol. 2023 Mar 14;25(3):566-579.
A549 cells
10 nM and 100 nM
To evaluate the inhibitory activity of Ulixertinib against ERK1 and ERK2, results showed IC50 values of 15 nM for ERK1 and 12 nM for ERK2
Chem Sci. 2018 Feb 6;9(9):2419-2431.
Ulixertinib HCl 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
MIA Paca-2 and HPNE-KRASG12D subcutaneous xenograft models
Oral
100mg/kg
Twice daily, until tumors reached maximum volume
To test the effect of Ulixertinib alone or in combination with gemcitabine on MIA Paca-2 and HPNE-KRASG12D subcutaneous xenografts, results showed that the combination treatment significantly suppressed tumor growth
Mol Cancer Ther. 2018 Oct;17(10):2144-2155
Rats mice
BT40 Xenograft Model
Oral
80 mg/kg
Twice daily for five consecutive days
Ulixertinib exhibited significant antitumoral activity in the BT40 xenograft model, significantly prolonging mouse survival.
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