1188296-52-7
中文名称
无中文名称
英文名称
PF 4800567 hydrochloride
CAS
1188296-52-7
分子式
C17H18ClN5O2
分子量
359.81
MOL 文件
1188296-52-7.mol
更新日期
2024/04/29 17:03:06
1188296-52-7 结构式
基本信息
中文别名
化合物PF-4800567PF-4800567游离态
3-[(3-氯苯氧基)甲基]-1-(四氢-2H-吡喃-4-基)-1H-吡唑并[3,4-D]嘧啶-4-胺
英文别名
PF 4800567PF 4800567
PF-4800567
PF 4800567 hydrochloride
3-[(3-chlorophenoxy)methyl]-1-(oxan-4-yl)pyrazolo[3,4-d]pyrimidin-4-amine
3-[(3-Chlorophenoxy)methyl]-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 3-[(3-chlorophenoxy)methyl]-1-(tetrahydro-2H-pyran-4-yl)-
3-[(3-Chlorophenoxy)Methyl]-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyriMidin-4-aMine Hydrochloride
所属类别
生物：小分子化合物物理化学性质
沸点592.9±50.0 °C(Predicted)
密度1.52±0.1 g/cm3(Predicted)
储存条件Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度DMF: 25 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 10 mg/ml; Ethanol: 1 mg/ml
酸度系数(pKa)4.01±0.30(Predicted)
形态结晶固体
应用领域
用途1
PF 4800567 is a selective casein kinase 1蔚 inhibitor; displays 22-fold greater potency towards CK1蔚 than CK1δ (IC50 values are 32 and 711 nM for CK1蔚 and CK1δ respectively). ATP competitive. Displays
minimal effect on the circadian clock.常见问题列表
生物活性
PF 4800567是casein kinase 1 epsilon (IC50=32 nM) 的新型有效抑制剂，其选择性是casein kinase 1 delta(IC50=711 nM)的20倍以上。靶点
| Target | Value |
|
casein kinase 1 epsilon
(Cell-free assay) | 32 nM |
|
casein kinase 1 delta
() | 711 nM |
体外研究
PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC 50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC 50 , 711 nM). PF-4800567 shows inhibitory activity against CK1ϵ and CK1δ in whole cells, with IC 50 s of 2.65 and 20.38 μM, respectively. PF-4800567 (0.01-10 μM) blocks CK1ϵ-mediated PER3 nuclear localization mediated by CK1ϵ and suppresses PER2 degradation at 1 μM. In addition, PF-4800567 has little effect on the circadian clock at 32 nM.
体内研究
PF-4800567 (100 mg/kg, s.c.) is rapidly absorpted and distributed in plasma and brain of mice.