CZC-54252
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CAS No. | 1191911-27-9 | Cat. No. | BCP15148 |
Related Products | 1784253-05-9(CZC 54252 hydrochloride) | ||
Name | CZC-54252 | ||
Synonyms | CZC54252;CZC 54252; | ||
SMILES | CS(=O)(NC1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCOCC4)C=C3OC)=NC=C2Cl)=O | ||
Chemical Name | |||
Formula | C22H25ClN6O4S | M. Wt | 504.99 |
Purity | 98% | Storage | Store at 4-8°C |
Description | 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. |
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