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VRT752271(HCl)

(CAS No:869886-67-9)
Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
CAS No:869886-67-9
Molecular Weight(MW):433.33
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 869886-67-9
Molecular formula(MF) C21H22Cl2N4O2
Molecular Weight(MW): 433.33
Alias
Solubility
In vitro DMSO 86 mg/mL (198.46 mM)
Ethanol 15 mg/mL (34.61 mM)
Water <1 mg/mL
In vivo
Biological Activity
Description Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Targets
ERK1 [1] ERK2 [1]
<0.3 nM
In vitro

In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A375 cells Function assay 2 h Inhibition of ERK1/2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-RSK level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50=0.14 μM 25977981
human A375 cells Proliferation assay 72 h Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant after 72 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50=0.18 μM 25977981

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