1. JAK/STAT Signaling
    Apoptosis
  2. Pim
    Apoptosis
  3. PIM-447 dihydrochloride

PIM-447 dihydrochloride (Synonyms: LGH447 dihydrochloride)

Cat. No.: HY-19322B Purity: 99.33% ee.: 100.00%
Handling Instructions

PIM447 dihydrochloride (LGH447 dihydrochloride) 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 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis.

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

PIM-447 dihydrochloride Chemical Structure

PIM-447 dihydrochloride Chemical Structure

CAS No. : 1820565-69-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 418 In-stock
Estimated Time of Arrival: December 31
1 mg USD 135 In-stock
Estimated Time of Arrival: December 31
5 mg USD 370 In-stock
Estimated Time of Arrival: December 31
10 mg USD 630 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2850 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of PIM-447 dihydrochloride:

Top Publications Citing Use of Products

    PIM-447 dihydrochloride purchased from MCE. Usage Cited in: J Pathol. 2020 Sep;252(1):65-76.

    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.
    • Biological Activity

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    • Customer Review

    Description

    PIM447 dihydrochloride (LGH447 dihydrochloride) 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 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis[1][2].

    In Vitro

    PIM-447 (0.05-10 µM; 24, 48 and 72 hours)has inhibitory effects in MM cells, it against sensitive cell lines with IC50 values 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 h >7 µM (OPM-2,RPMI-LR5, U266-Dox4 and U266-LR7)[1].
    PIM-447 (0.1-10 µM; 24, 48 and 72 hours) does not induce important levels of apoptosis, when PIM447 at 5 µM, it substantially increases annexin-V levels (about 30%) in sensitive cell lines(MM1S, NCI-H929 and RPMI-8226).when PIM447 at 10 µM, it induces apoptosis in all the cell lines but to a lesser extent in OPM-2 and RPMI-LR5[1].
    PIM447 promotes the cleavage of initiator caspases, such as caspases 8 and 9, and increases the cleavage of the effector caspases 3 and 7, together with PARP cleavage in MM1S,RPMI-8226 and NCI-H929 cells[1].
    PIM447 (0.1-1 µM) increases the percentage of cells in the G0/G1 phase and decreases the proliferative phases (S and G2/M) of the cell cycle. The effects at low concentrations (0.1-1 µM) were more pronounced in MM1S cells than in OPM-2[1].

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

    Cell Viability Assay[1]

    Cell Line: Sensitive MM cell lines: MM1S, MM1R, RPMI-8226, MM144, U266 and NCI-H929 cells
    Less sensitive MM cell lines: OPM-2,RPMI-LR5, U266-Dox4 and U266-LR7cells
    Concentration: 0.05-10 µM
    Incubation Time: 24, 48 and 72 hours
    Result: Was cytotoxic for MM cells (PIM kinases highly expressed).

    Apoptosis Analysis[1]

    Cell Line: Sensitive MM cell lines: MM1S, NCI-H929 and RPMI-8226 cells
    Less sensitive MM cell lines: OPM-2 and RPMI-LR5 cells
    Concentration: 0.05-10 µM
    Incubation Time: 24, 48 and 72 hours
    Result: Induced cell apoptosis at higer doses, had no effects at 0.1-1 uM.

    Western Blot Analysis[1]

    Cell Line: Sensitive MM cell lines: MM1S, NCI-H929 and RPMI-8226 cells
    Concentration: 0.05-10 µM
    Incubation Time: 24, 48 hours
    Result: Increased the cleavage of the effector caspases 3 and 7, and the PARP cleavage.

    Cell Cycle Analysis[1]

    Cell Line: MM1S, OPM-2 cells
    Concentration: 0.1, 0.5 or 1 µM
    Incubation Time: 48 hours
    Result: Increased the cleavage of the effector caspases 3 and 7, and the PARP cleavage.
    In Vivo

    PIM447 (oral gavage; 100 mg/kg; 5 times/week) clearly controlls tumor progression and the serum levels of hIgλ secreted by RPMI-8226-luc cells in mouse model of bone marrow-disseminated human multiple myeloma[1].

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

    Animal Model: RPMI-8226-luc cells are injected intravenously into 6-week-old female NODSCID-IL-2Rγ-/-(NSG) mice[1]
    Dosage: 100 mg/kg
    Administration: oral gavage; 100 mg/kg; 5 times/week
    Result: Was well tolerated, as the body weight of mice did not decrease by more than 10%.
    Increased bone volume density and trabecular number and reduced trabecular separation relative to vehicle group.
    Clinical Trial
    Molecular Weight

    513.38

    Formula

    C₂₄H₂₅Cl₂F₃N₄O

    CAS No.

    1820565-69-2

    SMILES

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

    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 : ≥ 46.7 mg/mL (90.97 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9479 mL 9.7394 mL 19.4787 mL
    5 mM 0.3896 mL 1.9479 mL 3.8957 mL
    10 mM 0.1948 mL 0.9739 mL 1.9479 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  1% DMSO    99% saline

      Solubility: ≥ 0.5 mg/mL (0.97 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

    • 4.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 5 mg/mL (9.74 mM); Clear solution

    • 5.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 5 mg/mL (9.74 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.33% ee.: 100.00%

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    Keywords:

    PIM-447LGH447PIM447PIM 447LGH 447LGH-447PimApoptosisPim kinasesMM1SMM1RRPMI-8226MM144U266NCI-H929OPM-2apoptosismultiple myelomabone marrowInhibitorinhibitorinhibit

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    Product Name:
    PIM-447 dihydrochloride
    Cat. No.:
    HY-19322B
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