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

Ulixertinib (Synonyms: BVD-523; VRT752271)

Cat. No.: HY-15816 Purity: 99.92%
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

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10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 110 In-stock
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50 mg USD 250 In-stock
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100 mg USD 450 In-stock
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200 mg USD 650 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Ulixertinib:

Top Publications Citing Use of Products

    Ulixertinib purchased from MCE. Usage Cited in: Innate Immun. 2020 Aug;26(6):505-513.

    The protein levels of p-ERK1/2, ERK1/2, p-RSK, and RSK are measured by Western blotting.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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

    ERK2

    0.3 nM (IC50, at KM ATP (60 μM))

    ERK1

     

    In Vitro

    Combined Ulixertinib (BVD-523; 10, 20, 30 μM; 48 hours) and VS-5584 treatment causes significant induction of cell death in human pancreatic cancer (HPAC) cells in PDAC cell lines BxPC-3, MIAPaCa-2, and CFPAC-1[3].

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

    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].

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

    Clinical Trial
    Molecular Weight

    433.33

    Formula

    C₂₁H₂₂Cl₂N₄O₂

    CAS No.
    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 : 100 mg/mL (230.77 mM; Need ultrasonic)

    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:  1% (w/v) carboxymethylcellulose (CMC)

      Solubility: 10 mg/mL (23.08 mM); Suspended solution; Need ultrasonic

    • 2.

      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

    • 3.

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

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

    • 4.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

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

    • 5.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

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

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

    Purity: 99.92%

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    Keywords:

    UlixertinibBVD-523 VRT752271BVD523BVD 523VRT752271VRT 752271VRT-752271ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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