1883548-84-2
1883548-84-2 structure
- Name: AMG PERK 44
- Chemical Name: AMG PERK 44
- CAS Number: 1883548-84-2
- Molecular Formula: C34H29ClN4O2
- Molecular Weight: 561.07
- Catalog: Signaling Pathways Cell Cycle/DNA Damage PERK
- Create Date: 2020-01-23 23:27:51
- Modify Date: 2024-01-08 20:35:06
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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[1][2].
| Name | AMG PERK 44 |
|---|
| Description | 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[1][2]. |
|---|---|
| Related Catalog | |
| 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]. Animal Model: Four- to six-week old naive athymic nude mice[1] Dosage: 3, 10, 30, 100 mg/kg Administration: Orally Result: Robustly inhibited PERK autophosphorylation in this assay (ED50=3 mg/kg; ED90=60 mg/kg at the 4 hours time point). Animal Model: Sprague-Dawley rats and male CD-1 mice[1] Dosage: 1 mg/kg (Pharmacokinetic Analysis) Administration: Iv Result: Had a CL of 1.6 L/h•kg, a Vss of 3.6 L/kg and a MRT of 2.3 hours. |
| References |
| Molecular Formula | C34H29ClN4O2 |
|---|---|
| Molecular Weight | 561.07 |