AMG PERK 44 is an orally active and selective PERK inhibitor (IC50: 6 nM) and induces autophagy. It has 1000-fold and 160-fold selectivity over GCN2 (IC50: 7300 nM) and B-Raf (IC50 >1000 nM), respectively.

AMG PERK 44 shows an inhibitory for cell pPERK (IC50: 84 nM ) [1].

AMG PERK 44 (orally; 3-100 mg/kg) robustly inhibits PERK autophosphorylation (ED50: 3 mg/kg; ED90: 60 mg/kg at the 4 hours time point), and >50% target coverage is maintained for 24 h in a time course PD assay when dosed at 100 mg/kg p.o. AMG PERK 44 (iv; 1 mg/kg) has a CL of 1.6 L/h?kg, a Vss of 3.6 L/kg, and MRT of 2.3 hours in Sprague-Dawley rats and male CD-1 mice [1].

1883548-84-2

C34H29ClN4O2

561.07

AMG PERK 44

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years