Basic information Safety Supplier Related

LY 2606368

Basic information Safety Supplier Related

LY 2606368 Basic information

Product Name:
LY 2606368
Synonyms:
  • LY 2606368
  • 5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile LY2606368
  • 5-[[5-[2-(3-Aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-2-pyrazinecarbonitrile
  • 5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile
  • Prexasertib
  • LY 2606368;LY-2606368;PREXASERTIB
  • Prexasertib (LY2606368)
  • CS-1453
CAS:
1234015-52-1
MF:
C18H19N7O2
MW:
365.39
Mol File:
1234015-52-1.mol
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LY 2606368 Chemical Properties

Boiling point:
608.5±55.0 °C(Predicted)
Density 
1.37±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
insoluble in DMSO
form 
A crystalline solid
pka
11.89±0.10(Predicted)
color 
Light yellow to brown
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LY 2606368 Usage And Synthesis

Description

LY2606368 is a checkpoint kinase 1 (Chk1) inhibitor with a Ki value of 0.9 nM against the purified target and IC50 values of <13 nM in a viability study of multiple colorectal cancer cell lines. Inhibition of Chk1 causes double-strand DNA breakage in cells leading to an excessive cell damage burden and subsequent cell death. In vitro, LY2606368 inhibits the doxorubicin-activated G2/M checkpoint in p53-deficient HeLa cells with an EC50 value of 9 nM. LY2606368, at 25 nM, also significantly induces apoptosis and inhibits colony formation in AGS and MKN1 gastric cancer cells.

Uses

LY 2606368 is a novel CHK1 inhibitor under investigation as a chemopotentiating agent. It causes double-stranded DNA breakage while simultaneously removing the protection of the DNA damage checkpoints. LY 2606368 is representative of a novel class of drugs for the treatment of cancer and tumor growth inhibition.

References

[1] wu w, bi c, bence a k, et al. antitumor activity of chk1 inhibitor ly2606368 as a single agent in sw1990 human pancreas orthotopic tumor model. cancer research, 2012, 72(8 supplement): 1776.
[2] lainchbury m, matthews t p, mchardy t, et al. discovery of 3-alkoxyamino-5-(pyridin-2-ylamino) pyrazine-2-carbonitriles as selective, orally bioavailable chk1 inhibitors. journal of medicinal chemistry, 2012, 55(22): 10229-10240.
[3] mcneely s c, burke t f, durlandbusbice s, et al. abstract a108: ly2606368, a second generation chk1 inhibitor, inhibits growth of ovarian carcinoma xenografts either as monotherapy or in combination with standard-of-care agents. molecular cancer therapeutics, 2011, 10(supplement 1): a108.

LY 2606368Supplier

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