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

Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate 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 lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity.

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CAS No. : 2781996-46-9

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Prexasertib lactate Related Antibodies

Top Publications Citing Use of Products

33 Publications Citing Use of MCE Prexasertib lactate

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

    Prexasertib lactate 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 lactate 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 lactate 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 lactate 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 lactate 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 lactate 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 lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate 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 lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity[1][2].

    IC50 & Target

    Chk1

    <1 nM (IC50)

    Chk2

    8 nM (IC50)

    Clinical Trial
    Molecular Weight

    455.47

    Formula

    C21H25N7O5
    CAS No.
    SMILES

    OC([C@@H](O)C)=O.NCCCOC1=C(C2=CC(NC3=NC=C(C#N)N=C3)=NN2)C(OC)=CC=C1
    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 lactate 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:

    Prexasertib2781996-46-9LY2606368LY 2606368LY-2606368Checkpoint Kinase (Chk)ApoptosisDNA/RNA SynthesisATP-competitiveRSK1double-strandedDNAreplicationMELKSIKBRSK2ARK5CDC25ACDK2HeLaautophosphorylationS296S516H2AXHT-29Inhibitorinhibitorinhibit

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