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LY2603618 | Potent and selective Chk1 inhibitor

LY2603618 (911222-45-2) is a potent (IC50 = 7nM) and selective (>1000x over Chk2) Checkpoint kinase 1 (Chk1) inhibitor.1 Chk1 is an important regulator of the DNA damage response – combination treatment of LY2603618 with other chemotherapeutic agents significantly increased tumor growth inhibition when compared to chemotherapeutic alone.2,3,4 LY2603618 caused a dramatic suppression of cell growth in MCF-7 and MDA-MB-231 human breast cancer cells via Chk1 inhibition induced upregulation of replication stress caused by oncogenes.5


1) King et al. (2014), Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor; Invest. New Drugs, 32 213
2) Calvo et al. (2014), Preclinical analyses and phase I evaluation of LY2603618 administered in combination with pemetrexed and cisplatin in patients with advanced cancer; Invest. New Drugs, 32 955
3) Calvo et al. (2016), Phase I Study of CHK1 Inhibitor LY2603618 in Combination with Gemcitabine in Patients with Solid Tumors; Oncology, 91 251
4) Zhao et al. (2016), Inhibition of CHK1 enhances cell death induced by the Bcl-1-selective inhibitor ABT-199 in acute myeloid leukemia cells; Oncotarget, 7 34785
5) Zhang et al. (2016), Targeting radioresistant breast cancer cells by single agent CHK1 inhibitor via enhancing replication stress; Oncotarget, 7 34688

Focus Biomolecules reagent supplier, chemical structure of LY2603618 | Potent and selective Chk1 inhibitor | CAS 911222-45-2

Catalog#  10-4123-0005

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Catalog Number:
Potent and selective Chk1 inhibitor
Chemical Name:
Alternate Names:
Molecular Weight:
Molecular Formula:
Soluble in DMSO (up to 10 mg/ml)
Physical Properties:
Off-white solid
98% by HPLC
NMR (Conforms)
Storage Temperature:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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