1. JAK/STAT Signaling
    Apoptosis
  2. Pim
    Apoptosis
  3. PIM447

PIM447 (Synonyms: LGH447)

Cat. No.: HY-19322
Handling Instructions

PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis.

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

PIM447 Chemical Structure

PIM447 Chemical Structure

CAS No. : 1210608-43-7

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Top Publications Citing Use of Products

    PIM447 purchased from MCE. Usage Cited in: J Pathol. 2020 Jun 19.

    The alteration of MAPK/ERK pathway is validated by Western blotting with tumour lysates from the animal model, as illustrated by a downregulation of pERK1/2 in the PIM447 treatment group.
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    Description

    PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis[1][2].

    In Vitro

    PIM447 (0.05-10 μM; 24-72 hours) shows antiproliferative effect on the multiple myeloma (MM) cells[2].
    PIM447 (10 μM; 6-24 hours) induces apoptosis[2].
    PIM447 (0.1-10 μM; 48 hours) increases the percentage of cells in the G0-G1 phase and decreases the proliferative phases (S and G2–M) of the cell cycle, in the two cell lines (MM1S and OPM-2 cells) at all doses[2].

    Cell Viability Assay[2]

    Cell Line: MM1S, MM1R, RPMI-8226, MM144, U266, NCI-H929, OPM-2, RPMI-LR5, U266-Dox4, and U266-LR7 cells
    Concentration: 0.05, 0.1, 0.5, 1, 5, 10 μM
    Incubation Time: 24, 48, 72 hours
    Result: Sensitive cell lines with IC50 values at 48 hours ranging from 0.2 to 3.3 μM (MM1S, MM1R, RPMI-8226, MM144, U266, and NCI-H929) and less sensitive cell lines with IC50 values at 48 hours >7 μmol/L (OPM-2, RPMI-LR5, U266-Dox4, and U266-LR7).

    Western Blot Analysis[2]

    Cell Line: MM1S cells
    Concentration: 10 μM
    Incubation Time: 6, 12, 24 hours
    Result: Promoted the cleavage of initiator caspases, such as caspases 8 and 9, and also the cleavage of the effector caspases 3 and 7, together with PARP cleavage.
    In Vivo

    PIM447 (100 mg/kg; p.o.; 5 times for a week) reduces tumor burden[2].

    Animal Model: 6-week-old female NOD-SCID-IL-2Rγ−/− (NSG) mice (bearing RPMI-8226-luc cells)[2]
    Dosage: 100 mg/kg
    Administration: p.o.; 5 times for a week
    Result: Clearly controlled tumor progression as measured by bioluminescence. 
    Clinical Trial
    Molecular Weight

    440.46

    Formula

    C₂₄H₂₃F₃N₄O

    CAS No.

    1210608-43-7

    SMILES

    O=C(C1=CC=C(F)C(C2=C(F)C=CC=C2F)=N1)NC3=C([[email protected]@H]4C[[email protected]](C)C[[email protected]](N)C4)C=CN=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Keywords:

    PIM447LGH447PIM 447PIM-447LGH 447LGH-447PimApoptosisPim kinasespanantimyelomamultiplemyelomacellcycleapoptosistumorantiproliferativeprogressionbone-protectivehematologicalmalignanciesInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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