CZC-54252
| 中文名称 | CZC-54252 |
|---|---|
| 中文同义词 | N-(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;化合物CZC-54252 |
| 英文名称 | CZC-54252 |
| 英文同义词 | N-(2-(5-chloro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)phenyl)methanesulfonamide;CZC 54252 hydrochloride;CZC-54252;CS-1730;N-[2-[[5-Chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]methanesulfonamide hydrochloride;CZC 54252;CZC54252;CZC-54252, >98%;Methanesulfonamide, N-[2-[[5-chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]- |
| CAS号 | 1191911-27-9 |
| 分子式 | C22H25ClN6O4S |
| 分子量 | 504.99 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;抑制剂;小分子抑制剂，天然产物;Inhibitors |
| Mol文件 | 1191911-27-9.mol |
| 结构式 |  |
CZC-54252 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：20mg/mL； DMF:PBS(pH 7.2)(1:1)：0.5 mg/ml；二甲基亚砜：10mg/mL |
| 形态 | 粉末 |
| 酸度系数(pKa) | 8.50±0.10(Predicted) |
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。
| Target | Value |
|
LRRK2 (WT)
(Cell-free assay) | 1.28 nM |
|
LRRK2 (G2019S)
(Cell-free assay) | 1.85 nM |
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.
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