AZD0364 (ATG-017)

Catalog No.S8708 Batch:S870801

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Technical Data

Formula

C24H24F2N8O2
Molecular Weight 494.50 CAS No. 2097416-76-5
Solubility (25°C)* In vitro DMSO 99 mg/mL (200.2 mM)
Ethanol 99 mg/mL (200.2 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.49mg/ml Taking the 1 mL working solution as an example, add 50 μL of 9.8 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
4.95mg/ml Taking the 1 mL working solution as an example, add 50 μL of 99 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. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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

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].

Protocol (from reference)

Selleck's AZD0364 (ATG-017) has been cited by 11 publications

Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936] PubMed: 38588697
Conformation selection by ATP-competitive inhibitors and allosteric communication in ERK2 [ Elife, 2024, 12RP91507] PubMed: 38537148
Slowly progressive cell death induced by GPx4-deficiency occurs via MEK1/ERK2 activation as a downstream signal after iron-independent lipid peroxidation [ J Clin Biochem Nutr, 2024, 74(2):97-107] PubMed: 38510679
Investigating the Role of TGF-β Signaling Pathways in Human Corneal Endothelial Cell Primary Culture [ Cells, 2023, 12(12)1624] PubMed: 37371094
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] PubMed: 37620393
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] PubMed: 37620393
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] PubMed: 37620393
Conformation Selection by ATP-competitive Inhibitors and Allosteric Communication in ERK2 [ bioRxiv, 2023, 2023.09.12.557258] PubMed: 37745518
Non-canonical Targets of HIF1a Impair Oligodendrocyte Progenitor Cell Function [ Cell Stem Cell, 2021, 28(2):257-272.e11] PubMed: 33091368
Targeting the MAPK/ERK and PI3K/AKT Signaling Pathways Affects NRF2, Trx and GSH Antioxidant Systems in Leukemia Cells [ Antioxidants (Basel), 2020, 9(7)E633] PubMed: 32709140

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.