Name: Prexasertib (LY2606368)
Brand: Selleck Chemicals
SKU: S6385
Rating: 5 (13 reviews)

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

CAS: 1234015-52-1

Selleck's Prexasertib (LY2606368) has been cited by 13 publications

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

Related Targets	Chk1 Chk2	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	Click to Expand

Signaling Pathway

Chk Signaling Pathway

Choose Selective Chk Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

[1] David Hong, et al. J Clin Oncol. 2016 May 20;34(15):1764-71.

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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

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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