AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of mitogen-activated protein kinase 1
Product Description
Information
AZD0364 (ATG-017) AZD0364 (ATG-017) is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.
Targets
ERK2 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).
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.
Associated Targets(Human)
MAPK1TchemMitogen-activated protein kinase 1 (3 Activities)
1.Flemington V, Davies EJ, Robinson D, Sandin LC, Delpuech O, Zhang P, Hanson L, Farrington P, Bell S, Falenta K et al.. (2021) AZD0364 Is a Potent and Selective ERK1/2 Inhibitor That Enhances Antitumor Activity in KRAS-Mutant Tumor Models when Combined with the MEK Inhibitor, Selumetinib.. Mol Cancer Ther, 20 (2):(238-249). [PMID:33273059]
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