产品
编 号：F235579
分子式：C34H29ClN4O2
分子量：561.07
分子式：C34H29ClN4O2
分子量：561.07
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
结构图
CAS No: 1883548-84-2
产品详情
生物活性：
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.
体内研究：
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. 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. Animal Model:Four- to six-week old naive athymic nude mice
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
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.
体外研究：
AMG PERK 44 has an IC50 of 84 nM for cell pPERK.
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.
体内研究：
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. 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. Animal Model:Four- to six-week old naive athymic nude mice
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
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.
体外研究：
AMG PERK 44 has an IC50 of 84 nM for cell pPERK.
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