A Chk1 inhibitor
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LY2603618

Item No. 20351

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-bromo-4-methyl-2-[(2S)-2-morpholinylmethoxy]phenyl]-N'-(5-methyl-2-pyrazinyl)-urea
CAS Number
911222-45-2
Synonyms
  • IC-83
  • Rabusertib
Molecular Formula
C18H22BrN5O3
Formula Weight
436.3
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 10 mg/ml
λmax
212, 226, 254, 299 nm
SMILES
CC1=C(Br)C=C(NC(NC2=NC=C(C)N=C2)=O)C(OC[C@H]3OCCNC3)=C1
InChi Code
InChI=1S/C18H22BrN5O3/c1-11-5-16(27-10-13-8-20-3-4-26-13)15(6-14(11)19)23-18(25)24-17-9-21-12(2)7-22-17/h5-7,9,13,20H,3-4,8,10H2,1-2H3,(H2,22,23,24,25)/t13-/m0/s1
InChi Key
SYYBDNPGDKKJDU-ZDUSSCGKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $44

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    10 mg

    $80

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    25 mg

    $174

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    50 mg

    $260

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    Product Description

    LY2603618 is a checkpoint kinase 1 (Chk1) inhibitor (IC50 = 7 nM) that prevents the repair of DNA caused by DNA-damaging agents.1 It can inhibit Chk1 autophosphorylation and increase DNA damage-mediated Chk1 phosphorylation.2 LY2603618 has been used in xenograft tumor models to potentiate the antitumor efficacy of chemotherapeutic agents such as gemcitabine (Item No. 11690).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. King, C., Diaz, H., Barnard, D., et al. Characterization and preclinical development of LY2603618: A selective and potent Chk1 inhibitor. Invest New Drugs 32(2), 213-226 (2014).

    2. Wang, F.-Z., Fei, H.-r., Cui, Y.-J., et al. The checkpoint 1 kinase inhibitor LY2603618 induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Apoptosis 19(9), 1389-1398 (2014).

    3. Barnard, D., Diaz, H.B., Burke, T., et al. LY2603618, a selective CHK1 inhibitor, enhances the anti-tumor effect of gemcitabine in xenograft tumor models. Invest New Drugs 34(1), 49-60 (2016).