CZC 25146

Modify Date: 2024-01-10 22:16:35

CZC 25146 Structure
CZC 25146 structure
Common Name CZC 25146
CAS Number 1191911-26-8 Molecular Weight 488.535
Density 1.4±0.1 g/cm3 Boiling Point 697.4±65.0 °C at 760 mmHg
Molecular Formula C22H25FN6O4S Melting Point N/A
MSDS N/A Flash Point 375.5±34.3 °C

 Use of CZC 25146


CZC-25146 is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.IC50 value: 4.76 nM/6.87 nM(wild type/G2019S LRRK2) [1]Target: LRRK2 CZC-25146displayed a very clean profile, it inhibited only five kinases (PLK4, GAK, TNK1, CAMKK2 and PIP4K2C) with high potency, none of which have been classified as predictors of genotoxicity or hematopoietic toxicity. CZC-25146 neither caused cytotoxicity in human cortical neurons at concentrations below 5μM over a seven-day treatment in culture nor did it block neuronal development in vitro. CZC-25146 possesses favorable pharmacokinetic properties, such as a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/hr/kg that render it suitable for in-vivo studies.

 Names

Name N-(2-(5-fluoro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)phenyl)methanesulfonamide
Synonym More Synonyms

 CZC 25146 Biological Activity

Description CZC-25146 is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.IC50 value: 4.76 nM/6.87 nM(wild type/G2019S LRRK2) [1]Target: LRRK2 CZC-25146displayed a very clean profile, it inhibited only five kinases (PLK4, GAK, TNK1, CAMKK2 and PIP4K2C) with high potency, none of which have been classified as predictors of genotoxicity or hematopoietic toxicity. CZC-25146 neither caused cytotoxicity in human cortical neurons at concentrations below 5μM over a seven-day treatment in culture nor did it block neuronal development in vitro. CZC-25146 possesses favorable pharmacokinetic properties, such as a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/hr/kg that render it suitable for in-vivo studies.
Related Catalog
References

[1]. Ramsden N, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 697.4±65.0 °C at 760 mmHg
Molecular Formula C22H25FN6O4S
Molecular Weight 488.535
Flash Point 375.5±34.3 °C
Exact Mass 488.164215
PSA 126.09000
LogP 1.50
Vapour Pressure 0.0±2.2 mmHg at 25°C
Index of Refraction 1.655
Storage condition 2-8℃

 Synonyms

Methanesulfonamide, N-[2-[[5-fluoro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-
N-(2-(2-(2-Methoxy-4-morpholinophenylamino)-5-fluoropyrimidin-4-ylamino)phenyl)methanesulfonamide
N-{2-[(5-Fluoro-2-{[2-methoxy-4-(4-morpholinyl)phenyl]amino}-4-pyrimidinyl)amino]phenyl}methanesulfonamide
CZC-25146
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