AMG PERK 44
CAS No. : 1883548-84-2
| Size | Price | Stock |
|---|---|---|
| 5mg | $150 | In-stock |
| 10mg | $250 | In-stock |
| 25mg | $450 | In-stock |
| 50mg | $675 | In-stock |
| 100mg | $950 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-12661A |
| M.Wt: | 561.07 |
| Formula: | C34H29ClN4O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 25 mg/mL (ultrasonic) |
AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy[1][2].
IC50 & Target: IC50: 6 nM (PERK)[1]
In Vitro: AMG PERK 44 has an IC50 of 84 nM for cell pPERK[1].
In Vivo: AMG PERK 44 (orally; 3-100 mg/kg) robustly inhibits PERK autophosphorylation in this assay (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 po[1].
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].
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