A Chk1 inhibitor
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LY2606368

Item No. 21490

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-2-pyrazinecarbonitrile
CAS Number
1234015-52-1
Synonyms
  • Prexasertib
Molecular Formula
C18H19N7O2
Formula Weight
365.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
λmax
214, 295 nm
SMILES
NCCCOC1=C(C2=CC(N([H])C3=NC=C(C#N)N=C3)=NN2[H])C(OC)=CC=C1
InChi Code
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)
InChi Key
DOTGPNHGTYJDEP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $32

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    5 mg

    $104

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    10 mg

    $160

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    25 mg

    $280

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    Product 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.1,2 Inhibition of Chk1 causes double-strand DNA breakage in cells leading to an excessive cell damage burden and subsequent cell death.1,2 In vitro, LY2606368 inhibits the doxorubicin-activated G2/M checkpoint in p53-deficient HeLa cells with an EC50 value of 9 nM.1 LY2606368, at 25 nM, also significantly induces apoptosis and inhibits colony formation in AGS and MKN1 gastric cancer cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. King, C., Diaz, H.B., McNeely, S., et al. LY2606368 causes replication catastrophe and antitumor effects through CHK1-dependent mechanisms. Mol. Cancer Ther. 14(9), 2004-2013 (2015).

    2. Manic, G., Signore, M., Sistigu, A., et al. CHK1-targeted therapy to deplete DNA replication-stressed, p53-deficient, hyperdiploid colorectal cancer stem cells. Gut 67(5), 903-917 (2017).

    3. Yin, Y., Shen, Q., Zhang, P., et al. Chk1 inhibition potentiates the therapeutic efficacy of PARP inhibitor BMN673 in gastric cancer. Am. J. Cancer Res. 7(3), 473-483 (2017).