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

Ulixertinib (Synonyms: BVD-523; VRT752271)

Cat. No.: HY-15816 Purity: 99.87%
Handling Instructions

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. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line.

For research use only. We do not sell to patients.

Ulixertinib Chemical Structure

Ulixertinib 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 USD 77 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg USD 650 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

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. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line[1][2].

IC50 & Target[2]

ERK2

0.3 nM (IC50, at KM ATP (60 μM))

ERK1

 

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 Ulixertinib (VRT752271) in Balb/C mice[2].

Clinical Trial
Molecular Weight

433.33

Formula

C₂₁H₂₂Cl₂N₄O₂

CAS No.

869886-67-9

SMILES

O=C(C1=CC(C2=CC(NC(C)C)=NC=C2Cl)=CN1)N[[email protected]@H](C3=CC=CC(Cl)=C3)CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 45 mg/mL (103.85 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

UlixertinibBVD-523VRT752271BVD523BVD 523VRT 752271VRT-752271ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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Ulixertinib
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HY-15816
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