AMG PERK 44
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- CAS號:
- 1883548-84-2
- 英文名:
- AMG PERK 44
- 英文別名:
- AMG PERK 44;4-(2-Amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl)-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one hydrochloride;4-(2-Amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl)-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one hydrochloride , AMG PERK 44
- 中文名:
- AMG PERK 44
- 中文別名:
- 化合物 T10299;化合物 AMG PERK 44;4-(2-氨基-4-甲基-3-(2-甲基喹啉-6-基)苯甲?；?-1-甲基-2,5-二苯基-1,2-二氫-3H-吡唑-3-酮鹽酸鹽
- CBNumber:
- CB64919953
- 分子式:
- C34H29ClN4O2
- 分子量:
- 561.08
- MOL File:
- 1883548-84-2.mol
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AMG PERK 44化學(xué)性質(zhì)
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儲存條件:
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Store at -20°C
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溶解度:
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DMSO: 25 mg/mL (44.56 mM)
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形態(tài):
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Solid
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顏色:
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Light yellow to yellow
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AMG PERK 44性質(zhì)、用途與生產(chǎn)工藝
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 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)。
AMG PERK 44 has an IC
50
of 84 nM for cell pPERK.
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.
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Animal Model:
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Four- to six-week old naive athymic nude mice
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Dosage:
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3, 10, 30, 100 mg/kg
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Administration:
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Orally
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Result:
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Robustly inhibited PERK autophosphorylation in this assay (ED
50
=3 mg/kg; ED
90
=60 mg/kg at the 4 hours time point).
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Animal Model:
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Sprague-Dawley rats and male CD-1 mice
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Dosage:
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1 mg/kg (Pharmacokinetic Analysis)
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Administration:
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Iv
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Result:
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Had a CL of 1.6 L/h?kg, a V
ss
of 3.6 L/kg and a MRT of 2.3 hours.
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AMG PERK 44
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS編號 | 包裝 | 價格 |
|---|
| 2025/05/22 | HY-12661A | AMG PERK 44
AMG PERK 44 | 1883548-84-2 | 5mg | 990元 |
| 2025/05/22 | HY-12661A | AMG PERK 44
AMG PERK 44 | 1883548-84-2 | 10 mM * 1 mLin DMSO | 1222元 |
1883548-84-2, AMG PERK 44 相關(guān)搜索:
- 抑制劑
- 化合物 AMG PERK 44
- 4-(2-氨基-4-甲基-3-(2-甲基喹啉-6-基)苯甲?；?-1-甲基-2,5-二苯基-1,2-二氫-3H-吡唑-3-酮鹽酸鹽
- 化合物 T10299
- 1883548-84-2
- 4-(2-Amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl)-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one hydrochloride
- 4-(2-Amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl)-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one hydrochloride , AMG PERK 44
- AMG PERK 44