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    Ulixertinib (BVD-523; VRT752271)
    Ulixertinib (BVD-523; VRT752271)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0470
    CAS #: 869886-67-9Purity ≥98%

    Description: Ulixertinib (formerly also known as BVD-523 and VRT752271) is a novel, potent, orally bioactive, highly selective, ATP-competitive and reversible ERK1/ERK2 inhibitor with potential antineoplastic activity. It inhibits ERK2 with an IC50 of<0.3 nM. Ulixertinib is being developed by BioMed Valley Discoveries (BVD) for the treatment of myeloid leukaemia or myelodysplastic syndrome. In Sep 2020, the US FDA granted ulixertinib (BVD-523) an immediate Expanded Access Program (EAP). Downmodulation of ERK protein kinase activity inhibits VEGF secretion by human myeloma cells and myeloma-induced angiogenesis. Upon oral administration, BVD-523 inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways.

    References: J Med Chem. 2015 Jun 11;58(11):4790-801.

    Related CAS #: 1956366-10-1 (HCl)   869886-67-9 (free base)   1975172-95-2 (HCl hydrate)  

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    Molecular Weight (MW)433.33
    FormulaC21H22Cl2N4O2
    CAS No.869886-67-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 86 mg/mL (198.5 mM)
    Water: <1 mg/mL
    Ethanol: 15 mg/mL (34.6 mM)
    Other info

    Chemical Name: (S)-4-(5-chloro-2-(isopropylamino)pyridin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide.

    InChi Key: KSERXGMCDHOLSS-LJQANCHMSA-N

    InChi Code: InChI=1S/C21H22Cl2N4O2/c1-12(2)26-20-8-16(17(23)10-25-20)14-7-18(24-9-14)21(29)27-19(11-28)13-4-3-5-15(22)6-13/h3-10,12,19,24,28H,11H2,1-2H3,(H,25,26)(H,27,29)/t19-/m1/s1

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

    Synonyms BVD-523, VRT752271; BVD 523, BVD523, VRT-752271, VRT 752271, Ulixertinib


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.


    Cell Assay: 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.

    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

    Animal modelMice
    Formulation & DosageN/A
    References

    J Med Chem. 2015 Jun 11;58(11):4790-801


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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