1883548-84-2
中文名稱
AMG PERK 44
英文名稱
AMG PERK 44
CAS
1883548-84-2
分子式
C34H29ClN4O2
分子量
561.08
MOL 文件
1883548-84-2.mol
更新日期
2024/11/04 22:53:12
1883548-84-2 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 25 mg/mL (44.56 mM)
形態(tài)Solid
顏色Light yellow to yellow
常見(jiàn)問(wèn)題列表
生物活性
AMG PERK 44 是一種口服有效的，高選擇性的 PERK 抑制劑，IC50 為 6 nM。AMG PERK 44 對(duì) PERK 的選擇性分別是 GCN2 (IC50=7300 nM) 和 B-Raf (IC50 >1000 nM) 的 1000 倍和 160 倍。AMG PERK 44 可以誘導(dǎo)自噬 (autophagy)。靶點(diǎn)
IC50: 6 nM (PERK)
體外研究
AMG PERK 44 has an IC 50 of 84 nM for cell pPERK.
體內(nèi)研究
AMG PERK 44 (orally; 3-100 mg/kg) robustly inhibits PERK autophosphorylation in this assay (ED
50
=3 mg/kg; ED
90
=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 V
ss
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 (ED 50 =3 mg/kg; ED 90 =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 V ss of 3.6 L/kg and a MRT of 2.3 hours. |