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Experimental cancer drugs
Prexasertib
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    Prexasertib

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    Prexasertib
    Prexasertib.svg
    Clinical data
    Pregnancy
    category
    • IV
    ATC code
    • none
    Identifiers
    • 5-((5-(2-(3-Aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)-2-pyrazinecarbonitrile
    CAS Number
    ChemSpider
    UNII
    KEGG
    Chemical and physical data
    Formula C18H19N7O2
    Molar mass 365.397 g·mol−1
    3D model (JSmol)
    • C1=C(C(=C(C=C1)OC)C1=CC(=NN1)NC1=NC=C(N=C1)C#N)OCCCN
    • InChI=1S/C18H19N7O2/c1-26-14-4-2-5-15(27-7-3-6-19)18(14)13-8-16(25-24-13)23-17-11-21-12(9-20)10-22-17/h2,4-5,8,10-11H,3,6-7,19H2,1H3,(H2,22,23,24,25)
    • Key:DOTGPNHGTYJDEP-UHFFFAOYSA-N

    Prexasertib (LY2606368) is a small molecule checkpoint kinase inhibitor, mainly active against CHEK1, with minor activity against CHEK2. This causes induction of DNA double-strand breaks resulting in apoptosis. It was developed by Eli Lilly but the company announced in 2019 it was dropping prexasertib from active development, although clinical trials continue. Research continues into the efficacy of prexasertib in treatment of acute myeloid leukemia, myelodysplastic syndrome, rhabdomyosarcoma, and medulloblastoma.


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