1188296-52-7
中文名稱
無中文名稱
英文名稱
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
2024/12/23 17:38:48
1188296-52-7 結(jié)構(gòu)式
基本信息
中文別名
化合物PF-4800567PF-4800567游離態(tài)
3-[(3-氯苯氧基)甲基]-1-(四氫-2H-吡喃-4-基)-1H-吡唑并[3,4-D]嘧啶-4-胺
英文別名
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
所屬類別
生物：小分子化合物物理化學性質(zhì)
沸點592.9±50.0 °C(Predicted)
密度1.52±0.1 g/cm3(Predicted)
儲存條件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
酸度系數(shù)(pKa)4.01±0.30(Predicted)
形態(tài)結(jié)晶固體
顏色Light yellow to yellow
應用領域
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.常見問題列表
生物活性
PF 4800567是casein kinase 1 epsilon (IC50=32 nM) 的新型有效抑制劑，其選擇性是casein kinase 1 delta(IC50=711 nM)的20倍以上。靶點
| Target | Value |
|
casein kinase 1 epsilon
(Cell-free assay) | 32 nM |
|
casein kinase 1 delta
() | 711 nM |
體外研究
PF-4800567 is a potent and selective inhibitor of casein kinase 1? (CK1?), 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 CK1? and CK1δ in whole cells, with IC 50 s of 2.65 and 20.38 μM, respectively. PF-4800567 (0.01-10 μM) blocks CK1?-mediated PER3 nuclear localization mediated by CK1? and suppresses PER2 degradation at 1 μM. In addition, PF-4800567 has little effect on the circadian clock at 32 nM.
體內(nèi)研究
PF-4800567 (100 mg/kg, s.c.) is rapidly absorpted and distributed in plasma and brain of mice.