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

Prexasertib Mesylate Hydrate  (Synonyms: LY2606368 Mesylate Hydrate; LY2940930)

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

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CAS No. : 1234015-57-6

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Prexasertib Mesylate Hydrate Related Antibodies

Top Publications Citing Use of Products

33 Publications Citing Use of MCE Prexasertib Mesylate Hydrate

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

    Prexasertib Mesylate Hydrate 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 Mesylate Hydrate 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 Mesylate Hydrate 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 Mesylate Hydrate 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 Mesylate Hydrate 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 Mesylate Hydrate 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).

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    Description

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

    479.51

    Formula

    C19H25N7O6S
    CAS No.
    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    Prexasertib Mesylate Hydrate 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:

    Prexasertib Mesylate1234015-57-6LY2606368 Mesylate LY2940930LY2940930LY 2940930LY-2940930Checkpoint Kinase (Chk)ApoptosisATP-competitiveRSK1double-strandedDNAreplicationMELKSIKBRSK2ARK5CDC25ACDK2HeLaautophosphorylationS296S516H2AXHT-29Inhibitorinhibitorinhibit

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