LY2606368 - CAS 1234015-52-1
Catalog number: B0084-462722
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
Checkpoint Kinase (Chk)
Description:
LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-462722 10 mg $198 In stock
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Purity:
>98%
Appearance:
white solid powder
Synonyms:
LY-2606368; LY 2606368
MSDS:
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Current Developer:
Eli Lilly.
1.Phase I Study of LY2606368, a Checkpoint Kinase 1 Inhibitor, in Patients With Advanced Cancer.
Hong D1, Infante J2, Janku F2, Jones S2, Nguyen LM2, Burris H2, Naing A2, Bauer TM2, Piha-Paul S2, Johnson FM2, Kurzrock R2, Golden L2, Hynes S2, Lin J2, Lin AB2, Bendell J2. J Clin Oncol. 2016 Apr 4. pii: JCO645788. [Epub ahead of print]
PURPOSE: The primary objective was to determine safety, toxicity, and a recommended phase II dose regimen of LY2606368, an inhibitor of checkpoint kinase 1, as monotherapy.
2.LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms.
King C1, Diaz HB1, McNeely S1, Barnard D1, Dempsey J1, Blosser W1, Beckmann R1, Barda D2, Marshall MS3. Mol Cancer Ther. 2015 Sep;14(9):2004-13. doi: 10.1158/1535-7163.MCT-14-1037. Epub 2015 Jul 3.
CHK1 is a multifunctional protein kinase integral to both the cellular response to DNA damage and control of the number of active replication forks. CHK1 inhibitors are currently under investigation as chemopotentiating agents due to CHK1's role in establishing DNA damage checkpoints in the cell cycle. Here, we describe the characterization of a novel CHK1 inhibitor, LY2606368, which as a single agent causes double-stranded DNA breakage while simultaneously removing the protection of the DNA damage checkpoints. The action of LY2606368 is dependent upon inhibition of CHK1 and the corresponding increase in CDC25A activation of CDK2, which increases the number of replication forks while reducing their stability. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population. Loss of the CHK1-dependent DNA damage checkpoints permits cells with damaged DNA to proceed into early mitosis and die.
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CAS 1234015-52-1 LY2606368

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