AMG PERK 44

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AMG PERK 44 是一种口服有效的，高选择性的 PERK 抑制剂，IC50 为 6 nM。AMG PERK 44 对 PERK 的选择性分别是 GCN2 (IC50=7300 nM) 和 B-Raf (IC50 >1000 nM) 的 1000 倍和 160 倍。AMG PERK 44 可以诱导自噬 (autophagy)。

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.

AMG PERK 44 has an IC50 of 84 nM for cell pPERK.

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:IvResult:Had a CL of 1.6 L/h?kg, a Vss of 3.6 L/kg and a MRT of 2.3 hours.

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Autophagy

Autophagy

Autophagy | PERK

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1883548-84-2

561.07

C34H29ClN4O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 25 mg/mL (44.56 mM; 超声助溶 )

Cl.Cc1ccc2cc(ccc2n1)-c1c(C)ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c1N

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(-20℃)

With Ice Pack

≥ 2 years