Home Cell Cycle Chk inhibitor GDC-0575 For research use only.

GDC-0575

Synonyms: ARRY-575, RG7741

GDC-0575 is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM.

GDC-0575 Chemical Structure

GDC-0575 Chemical Structure

CAS No. 1196541-47-5

Purity & Quality Control

GDC-0575 Related Products

Signaling Pathway

Chk Signaling Pathways

Chk Signaling Pathway

Biological Activity

Description GDC-0575 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
In vitro

GDC-0575 enhances the cytotoxicity of Cytarabine (AraC) in vitro[1].
Experimental Result Images Methods Biomarkers Images PMID
Western blot pCHK1 / pRPA2 / RPA2 / RRM2 / γH2AX / α-tub pCHK2 / pCHK1 / p53 / pRPA2 / RPA2 / RRM2 / γH2AX / α-tub tPARP / cPARP / γH2AX / Tubulin 31044505
Growth inhibition assay tumor volume 31044505
IHC H&E staining / PCNA expression H&E staining Small intestine / Colon 33897258
Immunofluorescence F4/80 / iNOS F4/80 / iNOS F4/80 / CCR2 F4/80 / CCR2 33897258
In Vivo
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01564251 Completed
Lymphoma Solid Tumor
Genentech Inc.
 March 23 2012 Phase 1

Chemical Information & Solubility

Molecular Weight 378.27 Formula

C16H20BrN5O
CAS No. 1196541-47-5 SDF --
Smiles C1CC(CN(C1)C2=C3C(=CNC3=NC=C2Br)NC(=O)C4CC4)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 75 mg/mL ( (198.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
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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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