1191911-27-9
中文名称
CZC-54252
英文名称
CZC-54252
CAS
1191911-27-9
分子式
C22H25ClN6O4S
分子量
504.99
MOL 文件
1191911-27-9.mol
更新日期
2024/08/11 21:06:44
1191911-27-9 结构式
基本信息
中文别名
化合物CZC-54252N-(2-((5-氯-2-((2-甲氧基-4-吗啉苯基)氨基)嘧啶-4-基)氨基)苯基)甲磺酸
英文别名
CS-1730CZC-54252
CZC-54252, >98%
CZC 54252
CZC54252
CZC 54252 hydrochloride
N-(2-(5-chloro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)phenyl)methanesulfonamide
N-{2-[(5-chloro-2-{[2-methoxy-4-(morpholin-4-yl)phenyl]amino}pyrimidin-4-yl)amino]phenyl}methanesulfonamide
Methanesulfonamide, N-[2-[[5-chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-
N-[2-[[5-Chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]methanesulfonamide hydrochloride
所属类别
生物化工：激动剂抑制剂物理化学性质
沸点718.1±70.0 °C(Predicted)
密度1.452±0.06 g/cm3(Predicted)
储存条件Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度DMF: 20 mg/mL; DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL; DMSO: 10 mg/mL
酸度系数(pKa)8.50±0.10(Predicted)
形态粉末
颜色White to off-white
常见问题列表
生物活性
CZC-54252是一种有效的LRRK2抑制剂，对人源野生型LRRK2和G2019S LRRK2的IC50分别为1.28 nM和1.85 nM。靶点
| Target | Value |
|
LRRK2 (WT)
(Cell-free assay) | 1.28 nM |
|
LRRK2 (G2019S)
(Cell-free assay) | 1.85 nM |
体外研究
CZC-54252 inhibits the activity of recombinant human wild-type LRRK2 with an IC
50
ranging from ～1 to ～5 nM. The G2019S mutant is inhibited with an IC
50
ranging from ～2 to ～7 nM in a TF-FRET assay. In addition, they are screened against a kinase panel of 185 kinases and exhibited good selectivity.
G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 with an EC
50
of ~1 nM and fully reversed to wild-type levels by CZC-54252 at concentration of 1.6 nM.