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PRT382

Chemical Structure : PRT382

CAS No.: 2242790-05-0

PRT382 (PRT-382)

Catalog No.: PC-49559Not For Human Use, Lab Use Only.

PRT382 (PRT-382) is a potent, selective and SAM-competitive PRMT5 inhibitor with IC50 of 2.8 nM in filtration binding assays with recombinant human PRMT5/MEP50 and histone H2A as the protein substrate.

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    Biological Activity

    PRT382 (PRT-382) is a potent, selective and SAM-competitive PRMT5 inhibitor with IC50 of 2.8 nM in filtration binding assays with recombinant human PRMT5/MEP50 and histone H2A as the protein substrate.
    PRT382 displays no significant activity against 38 other methyltransferases (e.g DNMTs, MLL1-4 complexes, EZH1 and EZH2 complexes, NRMTs, NSD, SUVs, SMYs, SETs, PRDM9), and other members of the PRMT family.
    PRT382 exhibits an IC50 of 27 nM in a reducing sDMA assay in the Granta-519 lymphoma cell line.
    PRT382 demonstrated anti-proliferative efficacy in the leukemia and lymphoma cell lines CCMCL-1, JVM-2, U-2932, RL, and KARPAS-422 with IC50 values of 0.01-0.5 uM.
    PRT382 demonstrated low clearance and high oral bioavailability in mice, rats, and dogs (F% = 70–80%), and high AUC levels (1175 h*kg*ng/mL/mg) in mice.|
    PRT382 demonstrated anti-proliferative potency in HG3 and Mec-1 cells when compared to SAM-competitive PRMT5 inhibitor compounds JNJ-64619178, LLY-283, and PF-06855800.
    PRT382 (10 mg/kg, 0.5% methylcellulose) displayed antileukemic activity in an aggressive model of CLL/RT.

    Physicochemical Properties

    M.Wt 441.27
    Formula C18H18Cl2N4O5
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (Z)-7-((2R,3R,4S,5R)-5-((R)-(3,4-dichlorophenyl)(hydroxy)methyl)-3,4-dihydroxytetrahydrofuran-2-yl)-1,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one O-methyl oxime

    References

    1. Hing ZA, et al. Nat Commun. 2023 Jan 6;14(1):97.
    2. Sloan SL, et al. Blood. 2023 Jun 2:blood.2022019419.

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