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

Prexasertib dihydrochloride  (Synonyms: LY2606368 dihydrochloride)

Cat. No.: HY-18174A Purity: 99.42%
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Prexasertib dihydrochloride (LY2606368 dihydrochloride) 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 dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity.

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

CAS No. : 1234015-54-3

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Customer Review

Based on 33 publication(s) in Google Scholar

Other Forms of Prexasertib dihydrochloride:

Prexasertib dihydrochloride Related Antibodies

Top Publications Citing Use of Products

33 Publications Citing Use of MCE Prexasertib dihydrochloride

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

    Prexasertib dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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:

    View All Isoforms
    Chk1 Chk2 BUBR1

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Prexasertib dihydrochloride (LY2606368 dihydrochloride) 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 dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride 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 dihydrochloride (LY2606368 dihydrochloride) inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), ARK5 (IC50=64 nM). LY2606368 requires CDC25A and CDK2 to cause DNA damage[1].
    ? Prexasertib dihydrochloride (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells[1].
    ? Prexasertib dihydrochloride (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells[1].
    ? Prexasertib dihydrochloride (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 dihydrochloride (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib (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 dihydrochloride 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 dihydrochloride (LY2606368 dihydrochloride; 1-10 mg/kg; SC; twice daily for 3 days, rest 4 days; for three cycles) causes growth inhibition in tumor xenografts[1].
    ? Prexasertib dihydrochloride (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

    438.31

    Formula

    C18H21Cl2N7O2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    NCCCOC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2.[H]Cl.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 8 mg/mL (18.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2815 mL 11.4075 mL 22.8149 mL
    5 mM 0.4563 mL 2.2815 mL 4.5630 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 (sealed storage, away from moisture). 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: ≥ 0.8 mg/mL (1.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.8 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.0 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: ≥ 0.8 mg/mL (1.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.8 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.0 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

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
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    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 (sealed storage, away from moisture)

    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: 99.73%

    SDS (393 KB)

    COA (257 KB) HNMR (146 KB) LCMS (101 KB) Elemental Analysis Report (115 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 2.2815 mL 11.4075 mL 22.8149 mL 57.0373 mL
    5 mM 0.4563 mL 2.2815 mL 4.5630 mL 11.4075 mL
    10 mM 0.2281 mL 1.1407 mL 2.2815 mL 5.7037 mL
    15 mM 0.1521 mL 0.7605 mL 1.5210 mL 3.8025 mL
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    Prexasertib dihydrochloride Related Classifications

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    • 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:

    Prexasertib1234015-54-3LY2606368LY 2606368LY-2606368Checkpoint Kinase (Chk)ApoptosisATP-competitiveRSK1double-strandedDNAreplicationMELKSIKBRSK2ARK5CDC25ACDK2HeLaautophosphorylationS296S516H2AXHT-29Inhibitorinhibitorinhibit

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