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AMG PERK 44
产品别名
1644664-21-0
AMG PERK 44
4-[2-Amino-4-methyl-3-(2-methyl-6-quinolinyl)benzoyl]-1,2-dihydro-1-methyl-2,5-diphenyl-3H-pyrazol-3-one hydrochloride
PERK inhibitor 44
4-(2-Amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl)-1-methyl-2,5-diphenyl-1H-pyrazol-3(2H)-one hydrochloride
AMG44
Compound 44
AMG′44
PERK-IN-1
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C34H28N4O2 · xHCl |
| Molecular weight | 524.61 (free base basis) |
| Biochem/physiol Actions【生化/生理作用】 | AMG PERK 44 (AMG44) is an orally active (F = 46% (mouse) & 55% (rat) post 2.5 mg/kg po.), active site-targeing, potent and highly selective PERK (EIF2AK3) inhibitor (IC50 = 6 nM; GCN2 IC50 = 7.3 μM, b-Raf IC50 >1 μM, <65% inhibition at 1 μM against 387 kinases). AMG44 inhibits cellular PERK autophosphorylation (pT980 IC50 = 84 nM; HT1080 T-REx-PERK-FLAG transfectants) and ER stress-induced bulk protein synthesis (IC50 = 400 nM; U2OS), as well as PERK pT980 in HT1080 Matrigel plug implant in mice in vivo (ED50 = 3 mg/kg & ED90 = 60 mg/kg 4 hr post po.). |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | −20℃ |
| SMILES string | O=C1N(N(C(C2=CC=CC=C2)=C1C(C3=CC=C(C(C4=CC=C5N=C(C=CC5=C4)C)=C3N)C)=O)C)C6=CC=CC=C6.[xHCl] |
