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AMG PERK 44

品牌
Sigma-Aldrich
CAS
1644664-21-0
货号
SML3049
规格纯度
≥98% (HPLC)
参考价格
1156.54 *本价格含增值税费
促销
服务
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  • 增值税票
数量
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产品名称:
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
产品介绍:

产品说明

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.).

基本信息

经验(实验)分子式C34H28N4O2 · xHCl
分子量524.61 (free base basis)

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
颜色 white to beige
溶解性DMSO: 2 mg/mL, clear
储存温度−20℃
SMILES stringO=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]

Sigma-Aldrich

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