2. Cell Cycle/DNA Damage Apoptosis
  3. Checkpoint Kinase (Chk) Apoptosis
  4. Prexasertib dimesylate

Prexasertib dimesylate  (Synonyms: LY2606368 dimesylate)

Cat. No.: HY-18174E Purity: 98.90%
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Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.

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

CAS No. : 1234015-58-7

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Based on 33 publication(s) in Google Scholar

Other Forms of Prexasertib dimesylate:

Prexasertib dimesylate Related Antibodies

Top Publications Citing Use of Products

33 Publications Citing Use of MCE Prexasertib dimesylate

Cell Proliferation/Viability Assay
WB
Flow Cytometry
In Vivo Efficacy Study
Apoptosis Analysis
RT-PCR

    Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111.  [Abstract]

    Full length and cleaved PARP protein expressions are determined by western blot in Hepa1-6 cells and Huh-7 cells induced by prexasertib with dose of 1 µM and 5 nM for 24 h, respectively.

    Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111.  [Abstract]

    Representative image of FACS analysis of late apoptotic Hepa1-6 cell rate treated by DMSO or prexasertib with dose of 1 µM for 24 h are shown.

    Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111.  [Abstract]

    Tumour growth curves (Mean ± SEM) of murine HCC model treated by vehicle (n = 8) or prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days, n = 8) are shown.

    Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111.  [Abstract]

    Prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days). Representative images of TUNEL assay for cellular apoptosis (green staining) in tumours are shown.

    Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111.  [Abstract]

    Prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days, n = 8). PD-L1 mRNA expression is determined by qPCR in tumours treated by prexasertib or vehicle.

    Prexasertib dimesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 2;10(1):3485.  [Abstract]

    Viability of mock control and Myc-activated CRISPRa cells upon treatment with 40 nM prexasertib for 96 h (n = 3).

    View All Checkpoint Kinase (Chk) Isoform Specific Products:

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    Chk1 Chk2 BUBR1

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity[1][2].

    IC50 & Target[1]

    Chk1

    0.9 nM (Ki)

    Chk1

    <1 nM (IC50)

    Chk2

    8 nM (IC50)

    In Vitro

    Prexasertib dimesylate (LY2606368 dimesylate) inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), ARK5 (IC50=64 nM). Prexasertib dimesylate requires CDC25A and CDK2 to cause DNA damage[1].
    Prexasertib dimesylate (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells[1].
    Prexasertib dimesylate (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells[1].
    Prexasertib dimesylate (4 nM; 24 hours) results in a large shift in cell-cycle populations from G1 and G2-M to S-phase with an accompanied induction of H2AX phosphorylation in U-2 OS cells[1].
    Prexasertib dimesylate (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib dimesylate (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA[1].

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

    Prexasertib dimesylate Related Antibodies

    Cell Cycle Analysis[1]

    Cell Line: HeLa cells
    Concentration: 33, 100 nM
    Incubation Time: For 7 hours
    Result: Had an IC50 of 37 nM and resulted in the G2-M population received DNA damage during S-phase but continued to progress through the cell cycle into an early mitosis.

    Western Blot Analysis[1]

    Cell Line: HT-29 cells
    Concentration: 8, 16, 31, 63, 125, 250 nM
    Incubation Time: Pre-treated for 15 minutes
    Result: Inhibited CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) (IC50 of less than 31 nM) in HT-29 cells.
    In Vivo

    Prexasertib dimesylate (LY2606368 dimesylate; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts[1].
    Prexasertib dimesylate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8)[1].

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

    Animal Model: Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]
    Dosage: 1, 3.3, or 10 mg/kg
    Administration: SC; twice daily for 3 days, rest 4 days; for three cycles
    Result: Caused statistically significant tumor growth inhibition (up to 72.3%).
    Animal Model: Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]
    Dosage: 15 mg/kg (Pharmacokinetic Analysis)
    Administration: SC (200 μL)
    Result: CHK1 was 7 ng/mL at 12 hours and 3 ng/mL by 24 hours in plasma exposures.
    Phosphorylation of both H2AX (S139) and RPA2 (S4/S8) was detectable at 4 hours, showing the rapid occurrence of DNA damage.
    Molecular Weight

    557.60

    Formula

    C20H27N7O8S2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    N#CC1=NC=C(NC2=NNC(C3=C(OC)C=CC=C3OCCCN)=C2)N=C1.CS(=O)(O)=O.CS(=O)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (179.34 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 1.7934 mL 8.9670 mL 17.9340 mL
    5 mM 0.3587 mL 1.7934 mL 3.5868 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 3.5 mg/mL (6.28 mM); Clear solution

      This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 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: ≥ 3.5 mg/mL (6.28 mM); Clear solution

      This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 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

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    (per animal)

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    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    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
    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, 6 months; -20°C, 1 month (stored under nitrogen). 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 1.7934 mL 8.9670 mL 17.9340 mL 44.8350 mL
    5 mM 0.3587 mL 1.7934 mL 3.5868 mL 8.9670 mL
    10 mM 0.1793 mL 0.8967 mL 1.7934 mL 4.4835 mL
    15 mM 0.1196 mL 0.5978 mL 1.1956 mL 2.9890 mL
    20 mM 0.0897 mL 0.4484 mL 0.8967 mL 2.2418 mL
    25 mM 0.0717 mL 0.3587 mL 0.7174 mL 1.7934 mL
    30 mM 0.0598 mL 0.2989 mL 0.5978 mL 1.4945 mL
    40 mM 0.0448 mL 0.2242 mL 0.4484 mL 1.1209 mL
    50 mM 0.0359 mL 0.1793 mL 0.3587 mL 0.8967 mL
    60 mM 0.0299 mL 0.1495 mL 0.2989 mL 0.7473 mL
    80 mM 0.0224 mL 0.1121 mL 0.2242 mL 0.5604 mL
    100 mM 0.0179 mL 0.0897 mL 0.1793 mL 0.4484 mL
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    Prexasertib dimesylate 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:

    Prexasertib dimesylate1234015-58-7LY2606368 dimesylateCheckpoint Kinase (Chk)ApoptosisATP-competitiveRSK1double-strandedDNAreplicationMELKSIKBRSK2ARK5CDC25ACDK2HeLaautophosphorylationS296S516H2AXHT-29Inhibitorinhibitorinhibit

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