CZC-54252
| CAS号 | 1191911-27-9 | 货号 | BCP15148 |
| 中文名 | CZC-54252 | ||
| 英文名 | CZC-54252 | ||
| 中文别名 | |||
| 英文别名 | CZC54252;CZC 54252; | ||
| 分子式 | C22H25ClN6O4S | 分子量 | 504.99 |
| 生物活性 | CZC-54252 inhibited the activity of recombinant human wild-type LRRK2 with an IC50 ranging from ～1 to ～5 nM. The G2019S mutant was inhibited with an IC50 ranging from ～2 to ～7 nM in a TF-FRET assay. In addition, they were screened against a kinase panel of 185 kinases and exhibited good selectivity. CZC-25146 (19) inhibited five other kinases, PLK4, GAK, TNK1, CAMKK2, and PIP4K2C, with high potency only, but none of them have been classified as predictors of genotoxicity or hematopoietic toxicity [1]. G2019S LRRK2-induced human neuronal injury was attenuated by CZC-25146 with an EC50 of ~4 nM (EC50 CZC-54252 ~1 nM) and fully reversed to wild-type levels by both compounds at concentrations as low as 8 nM (1.6 nM for CZC-54252) . in vivo: In vivo pharmacology established a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/h/kg for CZC-25146. | ||
| 上下游产品 | 1784253-05-9（CZC 54252 hydrochloride） | ||
| 信号通路 | Others Pathway | ||
| 靶 点 | LRRK2 | ||
结构式
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