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Prexasertib (LY2606368) CHK1 Inhibitor

Name: Prexasertib (LY2606368)
Brand: Selleck Chemicals
SKU: S6385
Availability: InStock
Rating: 5 (23 reviews)

Cat.No.S6385

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.

Chemical Structure

Molecular Weight: 365.39

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Quality Control

Batch: S638501 DMSO]Insoluble]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.39%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS/MSDS
Datasheet

99.39

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase
Other Chk Inhibitors	Prexasertib (LY2606368) Dihydrochloride CCT245737 (SRA737) AZD7762 Rabusertib (LY2603618) MK-8776 (SCH 900776) CHIR-124 PF-477736 BML-277 (Chk2 Inhibitor II) GDC-0575 BBI-355

Solubility

In vitro
Batch:

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.050mg/ml (0.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 1 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.050mg/ml (0.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 1 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	365.39	Formula	C₁₈H₁₉N₇O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1234015-52-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ACR 368			SMILES	COC1=C(C2=CC(=N[NH]2)NC3=CN=C(C=N3)C#N)C(=CC=C1)OCCCN

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	Chk1 (in cell-free assay) 1 nM Chk2 (in cell-free assay) 8 nM RSK1 (in cell-free assay) 9 nM
References	[1] https://pubmed.ncbi.nlm.nih.gov/27044938/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-02-20)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04095221	COMPLETED	Desmoplastic Small Round Cell Tumor; Rhabdomyosarcoma	Memorial Sloan Kettering Cancer Center	2019-09-17	PHASE1; PHASE2
NCT04023669	COMPLETED	Brain Tumor; Brain Tumor, Recurrent; Brain Tumor, Refractory; Brain Tumor, Pediatric; Medulloblastoma; Medulloblastoma Recurrent; Medulloblastoma, Non-WNT/Non-SHH; Medulloblastoma, Non-WNT/Non-SHH, Group 3; Medulloblastoma, Non-WNT/Non-SHH, Group 4; Brain Cancer; CNS Cancer; CNS Tumor; CNS Neoplasm	St. Jude Children's Research Hospital	2019-08-08	PHASE1
NCT02649764	COMPLETED	Chronic Myelomonocytic Leukemia; Recurrent Acute Myeloid Leukemia; Recurrent High Risk Myelodysplastic Syndrome; Refractory Acute Myeloid Leukemia; Refractory High Risk Myelodysplastic Syndrome	M.D. Anderson Cancer Center	2016-05-04	PHASE1
NCT04032080	COMPLETED	Triple Negative Breast Cancer	Baylor Research Institute	2019-09-05	PHASE2
NCT02203513	TERMINATED	Ovarian Cancer; Breast Cancer; Prostate Cancer	National Cancer Institute (NCI)	2015-01-20	PHASE2
NCT03495323	COMPLETED	Cancer	Dana-Farber Cancer Institute	2018-05-16	PHASE1

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