Home Cell Cycle Chk inhibitor - S6 Kinase inhibitor Prexasertib (LY2606368) For research use only.

Prexasertib (LY2606368)

Synonyms: ACR 368

Prexasertib (LY2606368, ACR 368) is a selective ATP competitor inhibitor of Chk1 and Chk2 with IC50s of 1 nM and 8 nM in cell-free assays, respectively. Prexasertib also inhibits RSK1 with an IC50 of 9 nM in cell-free assay.

Prexasertib (LY2606368) Chemical Structure

Prexasertib (LY2606368) Chemical Structure

CAS No. 1234015-52-1

Purity & Quality Control

Batch: S638501 DMSO]3 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.39%
99.39

Prexasertib (LY2606368) Related Products

Signaling Pathway

Chk Signaling Pathways

Chk Signaling Pathway

Biological Activity

Description

Prexasertib (LY2606368, ACR 368) is a selective ATP competitor inhibitor of Chk1 and Chk2 with IC50s of 1 nM and 8 nM in cell-free assays, respectively. Prexasertib also inhibits RSK1 with an IC50 of 9 nM in cell-free assay.
Targets
Chk1 [1]
(in cell-free assay)		 Chk2 [1]
(in cell-free assay)		 RSK1 [1]
(in cell-free assay)
1 nM 8 nM 9 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04095221 Active not recruiting
Desmoplastic Small Round Cell Tumor|Rhabdomyosarcoma
Memorial Sloan Kettering Cancer Center
 September 17 2019 Phase 1|Phase 2
NCT03495323 Completed
Cancer
Dana-Farber Cancer Institute|Eli Lilly and Company
 May 16 2018 Phase 1
NCT03414047 Completed
Ovarian Cancer
Eli Lilly and Company
 April 10 2018 Phase 2
NCT03057145 Completed
Solid Tumor
Geoffrey Shapiro MD PhD|Eli Lilly and Company|AstraZeneca|Dana-Farber Cancer Institute
 March 10 2017 Phase 1

Chemical Information & Solubility

Molecular Weight 365.39 Formula

C18H19N7O2
CAS No. 1234015-52-1 SDF --
Smiles COC1=C(C2=CC(=N[NH]2)NC3=CN=C(C=N3)C#N)C(=CC=C1)OCCCN
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 3 mg/mL ( (8.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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