Ulixertinib

SKU: orb1300149

Description

Ulixertinib (BVD-523) is a potent and reversible dual inhibitor of ERK1 and ERK2, exhibiting an IC50 below 0.3 nM for ERK2. It is widely used in preclinical cancer research to investigate MAPK pathway signaling in both cellular and animal models of various malignancies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 869886-67-9
• MW: 433.33
• Purity: 99.95% (May vary between batches)
• Formula: C₂₁H₂₂Cl₂N₄O₂
• SMILES: CC(C)Nc1cc(-c2c[nH]c(c2)C(=O)N[C@H](CO)c2cccc(Cl)c2)c(Cl)cn1
• Target: ERK
• Solubility: Ethanol:12 mg/mL (27.69 mM);DMSO:250 mg/mL (576.93 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:8 mg/mL (18.46 mM)

Bioactivity

• Target IC50:
  ERK2:<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.
• Cell Research:
  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.(Only for Reference)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ulixertinib, VRT 752271, VRT752271, VRT-752271, Inhibitor, Extracellular signal regulated kinases, ERK, ERK2, inhibit, BVD 523, BVD523, BVD-523

Compound Identifiers

PubChem CID

11719003