Formulation: A solid
Formal Name: 4-(2-amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl)-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one, hydrochloride
Purity: ≥98%
Formula Markup: C34H28N4O2• XHCl
Formula Weight: 561,1
Shelf life (days): 1460
Notes: AMG PERK 44 is a protein kinase R-like ER kinase (PERK) inhibitor (IC50 = 6 nM).{68767} It is selective for PERK over general control nonderepressible 2 kinase (GCN2) and B-RAF (IC50s = 7,300 and >1,000 nM, respectively). It inhibits PERK autophosphorylation in a cell-free assay (IC50 = 84 nM) and rescues protein synthesis in U2OS cells (EC50 = 400 nM). AMG PERK 44 (1, 3, 10, and 30 mg/kg) reduces intratumoral PERK autophosphorylation in a doxycycline-inducible PERK Matrigel™ plug assay.