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Prexasertib

From Wikipedia, the free encyclopedia
Prexasertib
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
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H19N7O2
Molar mass365.397 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,[1] although clinical trials continue. Research continues into the efficacy of prexasertib in treatment of acute myeloid leukemia, myelodysplastic syndrome, rhabdomyosarcoma, and medulloblastoma.[2]

References

[edit]
  1. ^ Al Idrus A (30 April 2019). "Lilly dumps phase 2 cancer drugs that survived previous cull". Fierce Biotech.
  2. ^ "Clinical Trials Using Prexasertib". National Cancer Institute, National Institutes of Health, U.S. Department of Health and Human Services.