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    PD318088
    PD318088

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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 #: V0460
    CAS #: 391210-00-7Purity ≥98%

    Description: PD318088 (PD-318088), an analog of PD184352, is a novel, potent and non-ATP competitive (allosteric) MEK1/2 inhibitor with potential anticancer activity. PD318088 has high anti-proliferative activity against various cancer cells.

    References: Nat Struct Mol Biol. 2004 Dec;11(12):1192-7.

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    Molecular Weight (MW)561.09
    FormulaC16H13BrF3IN2O4
    CAS No.391210-00-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 112 mg/mL (199.6 mM)
    Water: <1 mg/mL
    Ethanol: 14 mg/mL (25.0 mM)
    Other infoChemical Name: 5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzamide
    InChi Key: XXSSGBYXSKOLAM-UHFFFAOYSA-N
    InChi Code: InChI=1S/C16H13BrF3IN2O4/c17-10-4-9(16(26)23-27-6-8(25)5-24)15(14(20)13(10)19)22-12-2-1-7(21)3-11(12)18/h1-4,8,22,24-25H,5-6H2,(H,23,26)
    SMILES Code: O=C(NOCC(O)CO)C1=CC(Br)=C(F)C(F)=C1NC2=CC=C(I)C=C2F
    SynonymsPD 318088; PD318088; PD-318088


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    In Vitro

    In vitro activity: PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure.


    Kinase Assay: PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM.

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    ReferencesNat Struct Mol Biol. 2004 Dec;11(12):1192-7.


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

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