Home MAPK ERK inhibitor Ulixertinib (BVD-523) For research use only.

Ulixertinib (BVD-523)

Synonyms: VRT752271

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

Ulixertinib (BVD-523) Chemical Structure

Ulixertinib (BVD-523) Chemical Structure

CAS: 869886-67-9

Selleck's Ulixertinib (BVD-523) has been cited by 57 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Products often used together with Ulixertinib (BVD-523)

Encorafenib

Ulixertinib, Encorafenib, and Cetuximab combo inhibits tumor growth better in CRC with BRAFV600E mutations.

Knoerzer D, et al. Cancer Res (2023) 83 (7_Supplement): 2693.

SHP099

Ulixertinib and SHP099 inhibit downstream MAPK signaling in SK-N-AS and CHP-212 cells and result in tumor growth delay in xenograft mice model.

Valencia-Sama I, et al. Cancer Res. 2020 Aug 15;80(16):3413-3423.

Trametinib (GSK1120212)

Ulixertinib and Trametinib plus Trastuzumab deruxtecan are extremely effective and lead to complete tumor regression in all PDX models.

Bulle AS, et al. Cancer Res (2022) 82 (12_Supplement): 5333.

Palbociclib

Ulixertinib and Palbociclib exhibit significant inhibition of tumor growth in the MB1998 patient-derived xenograft (PDX) model.

Nassar KW, et al. Mol Cancer Ther. 2021 Oct;20(10):2049-2060.

Gemcitabine

Ulixertinib enhances Gemcitabine's pro-apoptotic effect in HPNE-KRAS G12D cells, effectively inhibiting tumor growth in MIA Paca-2 xenografts.

Jiang H, et al. Mol Cancer Ther. 2018 Oct;17(10):2144-2155.

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 Function assay Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated RSK levels, IC50 = 0.031 μM. 28376306
A375 Function assay 2 hrs 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
A375 Antiproliferative assay 72 hrs 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
SKCO1 Antiproliferative assay 72 hrs Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.356 μM. 28038940
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.468 μM. 28038940
SW620 Antiproliferative assay 72 hrs Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.499 μM. 28038940
AsPC1 Antiproliferative assay 72 hrs Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.849 μM. 28038940
NCI-H23 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant after 72 hrs by CellTiter-Glo assay, IC50 = 1 μM. 28038940
SW156 Antiproliferative assay 72 hrs Antiproliferative activity against human SW156 cells harboring wild type KRAS after 72 hrs by CellTiter-Glo assay, IC50 = 1.24 μM. 28038940
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay, IC50 = 2.231 μM. 28038940
A375 Function assay 2 hrs Inhibition of ERK2 in human A375 cells harboring B-RAF V600E mutant assessed as decrease in phospho-ERK2 level after 2 hrs by Cellomics ArrayScanTM VTI imaging analysis, IC50 = 4.1 μM. 25977981
A375 Function assay Inhibition of ERK2 in human A375 cells harboring BRAF V600E mutant assessed as decrease in phosphorylated ERK2 levels, IC50 = 4.1 μM. 28376306
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs in presence of IL-3 by CellTiter-Glo assay, IC50 = 8.608 μM. 28038940
Click to View More Cell Line Experimental Data

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 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]
Kinase Assay ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay
MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
Cell Research Cell lines A375 cells
Concentrations ~30 μM
Incubation Time 72 h
Method A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 µL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO2 in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 µM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 µL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-ERK / ERK / RRM2 28797284
Growth inhibition assay Cell viability 30771617
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04488003 Active not recruiting Advanced Solid Tumor|BRAF Gene Mutation|BRAF Gene Alteration|MEK Mutation|MEK Alteration|MAP2K1 Gene Mutation|MAP2K1 Gene Alteration|MAP2K2 Gene Mutation|MAP2K2 Gene Alteration BioMed Valley Discoveries Inc November 3 2020 Phase 2
NCT04145297 Active not recruiting Gastrointestinal Neoplasms University of Utah|BioMed Valley Discoveries Inc March 17 2020 Phase 1
NCT03698994 Active not recruiting Advanced Malignant Solid Neoplasm|Recurrent Ependymal Tumor|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Histiocytic and Dendritic Cell Neoplasm|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Solid Neoplasm|Recurrent Medulloblastoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Primary Malignant Central Nervous System Neoplasm|Recurrent Rhabdoid Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Refractory Ependymoma|Refractory Ewing Sarcoma|Refractory Glioma|Refractory Hepatoblastoma|Refractory Histiocytic and Dendritic Cell Neoplasm|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Germ Cell Tumor|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Primary Malignant Central Nervous System Neoplasm|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Wilms Tumor National Cancer Institute (NCI) November 14 2018 Phase 2
NCT03417739 Active not recruiting Uveal Melanoma Dana-Farber Cancer Institute|BioMed Valley Discoveries Inc March 26 2018 Phase 2
NCT02994732 Completed Healthy BioMed Valley Discoveries Inc January 2017 Phase 1

Chemical lnformation & Solubility

Molecular Weight 433.33 Formula

C21H22Cl2N4O2
CAS No. 869886-67-9 SDF Download Ulixertinib (BVD-523) SDF
Smiles CC(C)NC1=NC=C(C(=C1)C2=CNC(=C2)C(=O)NC(CO)C3=CC(=CC=C3)Cl)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 86 mg/mL ( (198.46 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble


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