2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. MLN0905

MLN0905 is a potent, orally active Polo-like kinase 1 (PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC50 value of 2 nM. MLN0905 can be used for the research of cancer.

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

CAS No. : 1228960-69-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of MLN0905:

MLN0905 Related Antibodies

Top Publications Citing Use of Products

    MLN0905 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Oct 23;14(10):695.  [Abstract]

    PLA assay between TRIM26 and GPX4 in U118 cells treated with onvansertib (2 nM) or MLN0905 (2 nM).

    View All Polo-like Kinase (PLK) Isoform Specific Products:

    View All Isoforms
    PLK1 PLK2 PLK3 PLK4

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    MLN0905 is a potent, orally active Polo-like kinase 1 (PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC50 value of 2 nM. MLN0905 can be used for the research of cancer[1][2].

    IC50 & Target[1]

    PLK1

    2 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HeLa EC50
    29 μM
    Compound: 12c, MLN0905
    Inhibition of PLK-1 T210D mutant in human HeLa cells assessed as inhibition of Cdc25c phosphorylation at Thr-96 after 2 hrs by immunostaining
    Inhibition of PLK-1 T210D mutant in human HeLa cells assessed as inhibition of Cdc25c phosphorylation at Thr-96 after 2 hrs by immunostaining
    		[PMID: 22070629]
    In Vitro

    MLN0905 (compound 12c) has inhibitory potency against PLK1 with an IC50 value of 2 nM[1].
    MLN0905 exhibits potent activities for Cdc25C with an EC50 value of 33 nM[1].
    MLN0905 shows inhibitory effects on HT29, HCT116, H460, and A375 cell lines with LD50 values of 22 nM, 56 nM, 89 nM and 34 nM, respectively[1].
    MLN0905 (125 nM) shows strong mitotic arrest and monopolar spindle formation in HT-29 cells[1].
    MLN0905 suppresses the growth of lymphoma cell lines with IC50 values ranging from 3 - 24 nM[2].

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

    MLN0905 Related Antibodies
    In Vivo

    MLN0905 (p.o.; 50 mg/kg) shows a high sustained PD response in nude mice HT29 xenograft tumors[1].
    MLN0905 (p.o.; 6.25, 12.5, 25, 50 mg/kg) exhibits significant antitumor activities in mice HT29 xenograft tumors[1].
    MLN0905 (p.o.; 0-14.5 mg/kg; daily, QD×3/week) has marked antitumor effects in kinds of lymphoma xenograft model[1][2].

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

    Animal Model: Tumor (HT29) xenograft model[1]
    Dosage: 0-50 mg/kg
    Administration: P.O; daily, QD×3/week
    Result: Observed antitumor activity, tumor stasis or regression and well-tolerated oral doses.
    Molecular Weight

    486.56

    Formula

    C24H25F3N6S
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    CC1=NC=C(CCCN(C)C)C=C1NC2=NC(C(C=CC(C(F)(F)F)=C3)=C3NC(C4)=S)=C4C=N2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (61.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0552 mL 10.2762 mL 20.5525 mL
    5 mM 0.4110 mL 2.0552 mL 4.1105 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.94%

    SDS (393 KB)

    COA (259 KB) HNMR (177 KB) LCMS (439 KB)

    Handling Instructions (2659 KB)
    References

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0552 mL 10.2762 mL 20.5524 mL 51.3811 mL
    5 mM 0.4110 mL 2.0552 mL 4.1105 mL 10.2762 mL
    10 mM 0.2055 mL 1.0276 mL 2.0552 mL 5.1381 mL
    15 mM 0.1370 mL 0.6851 mL 1.3702 mL 3.4254 mL
    20 mM 0.1028 mL 0.5138 mL 1.0276 mL 2.5691 mL
    25 mM 0.0822 mL 0.4110 mL 0.8221 mL 2.0552 mL
    30 mM 0.0685 mL 0.3425 mL 0.6851 mL 1.7127 mL
    40 mM 0.0514 mL 0.2569 mL 0.5138 mL 1.2845 mL
    50 mM 0.0411 mL 0.2055 mL 0.4110 mL 1.0276 mL
    60 mM 0.0343 mL 0.1713 mL 0.3425 mL 0.8564 mL
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    MLN0905 Related Classifications

    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:

    MLN09051228960-69-7MLN 0905MLN-0905Polo-like Kinase (PLK)oralPolo-like kinase 1 (PLK1)inhibitorycancerInhibitorinhibitorinhibit

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