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Chemical Structure| 869886-67-9 Chemical Structure| 869886-67-9

Structure of Ulixertinib
CAS No.: 869886-67-9

Chemical Structure| 869886-67-9

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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 <0.3 nM against ERK2. It inhibits phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.

Synonyms: BVD-523; VRT752271

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Product Details of Ulixertinib

CAS No. :869886-67-9
Formula : C21H22Cl2N4O2
M.W : 433.33
SMILES Code : O=C(C1=CC(C2=CC(NC(C)C)=NC=C2Cl)=CN1)N[C@@H](C3=CC=CC(Cl)=C3)CO
Synonyms :
BVD-523; VRT752271
MDL No. :MFCD22628898
InChI Key :KSERXGMCDHOLSS-LJQANCHMSA-N
Pubchem ID :11719003

Safety of Ulixertinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Ulixertinib

MAPK

Isoform Comparison

Biological Activity

Target
  • ERK2

    ERK2, IC50:<0.3 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
QBC939 cells 1 µM 24 h To investigate the effect of the ERK inhibitor ulixertinib on the proliferation and migration of QBC939 cells. Results showed that ERK inhibition could suppress the promotion of proliferation and migration induced by SPRY4 knockdown. PMC6921364
QBC939 cells 1 µM 24 h To investigate the effect of ulixertinib on the cell cycle distribution of QBC939 cells. Results showed that ulixertinib increased the percentage of cells in the G1 phase and decreased the percentage of cells in the S and G2/M phases. PMC6921364
OMM2.3 cells 2 μM 72 h To evaluate the anti-proliferative effect of Ulixertinib in combination with BIX01294 on OMM2.3 cells, the results showed that the combination significantly enhanced the anti-proliferative effect. PMC10935147

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
nude mice QBC939 cell xenograft model intraperitoneal injection 3 mg/kg once daily for 15 days To investigate the effect of FGF2 stimulation on the SPRY4-overexpressing QBC939 cell xenograft model. Results showed that SPRY4 overexpression repressed tumor volume and weight, while FGF2 addition reversed this effect. PMC6921364
Mice ES2 xenograft model Intraperitoneal injection 50 mg/kg Every other day for three weeks To evaluate the effect of ERK inhibition on tumor progression, results showed that Ulixertinib significantly slowed tumor growth PMC10709884
nude mice UM orthotopic model oral 50 mg/kg once daily for 21 days To evaluate the inhibitory effect of Ulixertinib alone and in combination with UNC0631 on UM tumor growth, the results showed that the combination significantly inhibited tumor growth. PMC10935147

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05804227 Gliomas EARLY_PHASE1 RECRUITING 2027-09-22 M D Anderson Cancer Center, Ho... More >>uston, Texas, 77030, United States Less <<
NCT03417739 Uveal Melanoma PHASE2 ACTIVE_NOT_RECRUITING 2025-08-31 Massachusetts General Hospital... More >>, Boston, Massachusetts, 02214, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02215, United States Less <<
NCT01781429 Advanced Solid Tumors PHASE1|PHASE2 COMPLETED 2025-09-18 UCLA Med-Hematology & Oncology... More >>, Los Angeles, California, 90095, United States|Yale Cancer Center, New Haven, Connecticut, 06520, United States|Florida Cancer Specialists and Research Group (Sarah Cannon Research Institute), Sarasota, Florida, 34232, United States|Massachusetts General Hospital (MGH), Boston, Massachusetts, 02114, United States|Washington University School of Medicine, Saint Louis, Missouri, 63110, United States|Memorial Sloan-Kettering Cancer Center, New York, New York, 10065, United States|Sarah Cannon Research Institute Hospital at Vanderbilt, Nashville, Tennessee, 37203, United States|Vanderbilt-Ingram Cancer Center, Nashville, Tennessee, 37212, United States|UT M.D Anderson Cancer Center, Houston, Texas, 77030, United States Less <<
NCT02296242 Acute Myelogenous Leukemia|Mye... More >>lodysplastic Syndrome Less << PHASE1|PHASE2 COMPLETED 2017-06-15 UCLA Medical Center, Los Angel... More >>es, California, 90024, United States|Winship Cancer Institute of Emory University, Atlanta, Georgia, 30322, United States|Roswell Park Cancer Institute, Buffalo, New York, 14263, United States|Perelman Center for Advanced Medicine, Philadelphia, Pennsylvania, 19104, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States Less <<
NCT06411821 Histiocytic Neoplasms PHASE2 RECRUITING 2025-05-27 Memorial Sloan Kettering Baski... More >>ng Ridge (Consent Only), Basking Ridge, New Jersey, 07920, United States|Memorial Sloan Kettering Monmouth (Limited Protocol Activities), Middletown, New Jersey, 07748, United States|Memorial Sloan Kettering Bergen (Consent Only), Montvale, New Jersey, 07645, United States|Memorial Sloan Kettering Suffolk-Commack (Consent Only), Commack, New York, 11725, United States|Memorial Sloan Kettering Westchester (Limited Protocol Activities), Harrison, New York, 10604, United States|Memorial Sloan Kettering Cancer Center (All Protocol Activities), New York, New York, 10065, United States|Memorial Sloan Kettering Nassau (Consent Only), Uniondale, New York, 11553, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.54mL

2.31mL

1.15mL

23.08mL

4.62mL

2.31mL

References

 

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