LY2603618 Inhibitor CAS No. 911222-45-2

Cat. No.	Name	Size	Price
KI1262	LY2603618	5 mg	$272
	LY2603618	10 mg	$432
	LY2603618	50 mg	$1552
	LY2603618	200 mg	$3952

Chemical Characteristic

Product Name	LY2603618
Synonyms	IC-83
CAS No.	911222-45-2
Molecular Weight	436.3
Formula	C₁₈H₂₂BrN₅O₃
Chemical Name	1-[5-bromo-4-methyl-2-[[(2S)-morpholin-2-yl]methoxy]phenyl]-3-(5-methylpyrazin-2-yl)urea
Smiles	N(C(=O)Nc1cnc(cn1)C)c1c(cc(c(c1)Br)C)OCC1CNCCO1
Chemical Structure

Biological activities

LY2603618 is a selective inhibitor of Chk1. Chk1 kinase phosphorylates cdc25, which is an important phosphatase in cell cycle control, particularly for entry into mitosis. LY2603618 binds to and blocks Chk1 activity, thereby potentiating the efficacy of various chemotherapeutic agents.^[1] LY2603618 can impair DNA synthesis, cause aberrant mitotic figures, and have synergistic activity with pemetrexed, especially in p53 mutant tumor cells.^[2] LY2603618 is predicted to enhance the effects of antimetabolites, such as gemcitabine.^[3] In non-small cell lung cancer xenograft models, LY2603618 inhibits tumor growth when administrated in combination with pemetrexed.^[4]

Protocols

In vivo: LY2603618 is dissolved in DMSO.^[2]

References

[1] Dai Y, et al. New insights into checkpoint kinase 1 in the DNA damage response signaling network. Clin Cancer Res. 2010, 16(2): 376-383. [2] Garon EB, et al. Mitotic inhibitors. J Thorac Oncol. 2011, 6(11 Suppl 4):S1791-1792. [3] Calvo E, et al. Abstract A94: Dose determination of LY2603618, a Chk1 inhibitor, administered in combination with gemcitabine in patients with advanced cancer. Molecular Cancer Therapeutics. 2011, 10 (11). [4] Govindan R, et al. Summary of presentation from the targeted therapy in lung cancer meeting. J Thorac Oncol. 2011, 6(11 Suppl 4): S1757.

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