Home MAPK ERK inhibitor AZD0364 (ATG-017) For research use only.

AZD0364 (ATG-017)

AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.

AZD0364 (ATG-017) Chemical Structure

AZD0364 (ATG-017) Chemical Structure

CAS: 2097416-76-5

Selleck's AZD0364 (ATG-017) has been cited by 5 publications

Purity & Quality Control

Batch: S870801 DMSO] 99 mg/mL] false] Ethanol] 99 mg/mL] false] Water] Insoluble] false Purity: 99.95%
99.95

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Biological Activity

Description AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.
Targets
ERK2 [1]
0.6 nM
In vitro
In vitro

AZD0364 exhibits high cellular potency against a direct downstream substrate on the MAPK pathway (e.g. inhibition of phospho-p90RSK1 in BRAFV600E mutant A375 cells, IC50 = 6 nM). The molecule is a highly selective kinase inhibitor (10/329 kinases tested are inhibited at >50% at a 1 µM) and has long residence time on the protein (as determined by SPR on human unphosphorylated-ERK2: pKd = 10; t1/2 = 277 mins)[2].
In Vivo
In vivo

AZD0364 has good oral pharmacokinetics across species. In xenograft models, AZD0364 inhibits phospho-p90RSK1 in tumors in a dose-dependent manner. AZD0364 induces regressions in the KRAS mutant NSCLC Calu 6 xenograft model. AZD0364 can also be combined safely and effectively with the MEK1/2 inhibitor selumetinib in KRAS mutant NSCLC xenograft models[2].

Chemical lnformation & Solubility

Molecular Weight 494.50 Formula

C24H24F2N8O2
CAS No. 2097416-76-5 SDF --
Smiles CC1=CN=C(N=C1C2=CN3CC(N(C(=O)C3=N2)CC4=CC(=C(C=C4)F)F)COC)NC5=CC=NN5C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 99 mg/mL ( (200.2 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 99 mg/mL

Water : Insoluble


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In vivo
Batch:

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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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