1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK

VRT752271 (Synonyms: Ulixertinib)

Cat. No.: HY-15816 Purity: 99.86%
Data Sheet SDS Handling Instructions

VRT752271 is a reversible, ATP-competitive inhibitor of ERK1 and ERK2 kinases, with IC50 of <0.3 nM against ERK2.

For research use only. We do not sell to patients.
VRT752271 Chemical Structure

VRT752271 Chemical Structure

CAS No. : 869886-67-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $110 In-stock
5 mg $100 In-stock
10 mg $150 In-stock
50 mg $400 In-stock
100 mg $600 In-stock
200 mg $950 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

VRT752271 is a reversible, ATP-competitive inhibitor of ERK1 and ERK2 kinases, with IC50 of <0.3 nM against ERK2.

IC50 & Target

IC50: <0.3 nM (ERK2)[2]

In Vivo

In the pharmacokinetic study, the sensitivity and specificity of the assay are found to be sufficient for accurately characterizing the plasma pharmacokinetics of VRT752271 in Balb/C mice[1].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.3077 mL 11.5386 mL 23.0771 mL
5 mM 0.4615 mL 2.3077 mL 4.6154 mL
10 mM 0.2308 mL 1.1539 mL 2.3077 mL
Kinase Assay
[2]

The MEK autophosphorylation assay is performed using the ADP Glo Kinase Assay kit. Activated MEK protein is expressed and purified in-house. Enzyme and substrate solutions are prepared in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01 % Tween 20. 6 nM MEK protein is prepared in assay buffer and 2 µL is dispensed into each well of a 384-well white small volume medium bind plate containing test and reference control compounds. Compound plates are dosed with a 12 point dose response curve from 10 µM down to 0.0625 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 15 minute pre-incubation of enzyme and compound at room temperature, 2 µL of a 20 µM Ultra Pure ATP solution in assay buffer is added to the wells, and the reaction is allowed to progress for 90 minutes at room temperature before the addition of 4 µL ADP Glo reagent R1 to quench the reaction. The plate is incubated at room temperature for 45 minutes before the addition of 8 µL Kinase Detection Reagent, and then the luminescence signal is allowed to equilibrate for 60 minutes before the plates are read on a Pherastar plate reader. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

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, sing 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 are 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

433.33

Formula

C₂₁H₂₂Cl₂N₄O₂

CAS No.

869886-67-9

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 45 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.86%

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Product Name:
VRT752271
Cat. No.:
HY-15816
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