2. PIM447

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.

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PIM447 Chemical Structure

PIM447 Chemical Structure

CAS No. : 1210608-43-7

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Based on 4 publication(s) in Google Scholar

Other Forms of PIM447:

PIM447 Related Antibodies

Top Publications Citing Use of Products

    PIM447 purchased from MedChemExpress. Usage Cited in: J Pathol. 2020 Sep;252(1):65-76.  [Abstract]

    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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    • Purity & Documentation

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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].

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

    PIM447 Related Antibodies

    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].

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

    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.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=C(F)C(C2=C(F)C=CC=C2F)=N1)NC3=C([C@@H]4C[C@H](C)C[C@H](N)C4)C=CN=C3
    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 (227.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2704 mL 11.3518 mL 22.7035 mL
    5 mM 0.4541 mL 2.2704 mL 4.5407 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    Purity & Documentation

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2704 mL 11.3518 mL 22.7035 mL 56.7588 mL
    5 mM 0.4541 mL 2.2704 mL 4.5407 mL 11.3518 mL
    10 mM 0.2270 mL 1.1352 mL 2.2704 mL 5.6759 mL
    15 mM 0.1514 mL 0.7568 mL 1.5136 mL 3.7839 mL
    20 mM 0.1135 mL 0.5676 mL 1.1352 mL 2.8379 mL
    25 mM 0.0908 mL 0.4541 mL 0.9081 mL 2.2704 mL
    30 mM 0.0757 mL 0.3784 mL 0.7568 mL 1.8920 mL
    40 mM 0.0568 mL 0.2838 mL 0.5676 mL 1.4190 mL
    50 mM 0.0454 mL 0.2270 mL 0.4541 mL 1.1352 mL
    60 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9460 mL
    80 mM 0.0284 mL 0.1419 mL 0.2838 mL 0.7095 mL
    100 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5676 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PIM4471210608-43-7LGH447PIM 447PIM-447LGH 447LGH-447Inhibitorinhibitorinhibit

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