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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 Î¼M	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 Î¼M	25977981

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