GDC-0575 (ARRY-575)

Catalog No.S8526 Synonyms: RG7741

For research use only.

GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM.

GDC-0575 (ARRY-575) Chemical Structure

CAS No. 1196541-47-5

Selleck's GDC-0575 (ARRY-575) has been cited by 4 Publications

Purity & Quality Control

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Biological Activity

Description GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM.
Targets
Chk1 [1]
(Cell-free assay)
1.2 nM
In vitro

GDC-0575 enhances the cytotoxicity of Cytarabine (AraC) in vitro[1].

Assay
Methods Test Index PMID
Western blot pCHK1 / pRPA2 / RPA2 / RRM2 / γH2AX / α-tub ; pCHK2 / pCHK1 / p53 / pRPA2 / RPA2 / RRM2 / γH2AX / α-tub ; tPARP / cPARP / γH2AX / Tubulin 31044505 31649026
Growth inhibition assay tumor volume 31044505
IHC H&E staining / PCNA expression ; H&E staining ; Small intestine / Colon 33897258 31044505
Immunofluorescence F4/80 / iNOS ; F4/80 / iNOS ; F4/80 / CCR2 ; F4/80 / CCR2 33897258
In vivo

GDC-0575 is a highly-selective oral small-molecule Chk1 inhibitor that results in tumor shrinkage and growth delay in xenograft models[2].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 75 mg/mL
(198.27 mM)
Water Insoluble
Ethanol '5 mg/mL

Chemical Information

Molecular Weight 378.27
Formula

C16H20BrN5O

CAS No. 1196541-47-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(CN(C1)C2=C3C(=CNC3=NC=C2Br)NC(=O)C4CC4)N

In vivo Formulation Calculator (Clear solution)

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

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01564251 Completed Drug: GDC-0575|Drug: Gemcitabine Lymphoma Solid Tumor Genentech Inc. March 23 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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