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CZC-25146 HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CZC-25146 HCl图片
CAS NO:1330003-04-7
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 525.0
Formula C22H26ClFN6O4S
CAS No.1330003-04-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>46 mg/mL
Water: <1 mg/mL
Ethanol:
SMILES CodeCS(=O)(NC1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCOCC4)C=C3OC)=NC=C2F)=O.Cl
SynonymsCZC25146 HCl; CZC 25146; CZC-25146
实验参考方法
In Vitro

In vitro activity:CZC-25146 is a potent, selective, and metabolically stable LRRK2 inhibitor (Leucine-rich repeat kinase-2) with IC50 of 4.76 nM and 6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively. CZC-25146 prevents mutant LRRK2-induced injury of cultured rodent and human neurons with mid-nanomolar potency. CZC-25146 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.


Kinase Assay: 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.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).


Cell Assay:

In VivoIn vivo pharmacology established a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/h/kg for CZC-25146 (19). Unfortunately, it exhibited a poor brain penetration of just 4%..
Animal model Mice
Formulation & Dosage
References ACS Chem Biol. 2011 Oct 21;6(10):1021-8.ACS Chem Biol. 2011 Oct 21;6(10):1021-8.