CZC-25146-d3

Modify Date: 2024-01-13 10:57:32

CZC-25146-d3 Structure
CZC-25146-d3 structure
Common Name CZC-25146-d3
CAS Number 1330003-04-7 Molecular Weight 525.00
Density 1.4±0.1 g/cm3 Boiling Point 697.4±65.0 °C at 760 mmHg
Molecular Formula C22H26ClFN6O4S Melting Point N/A
MSDS Chinese USA Flash Point 375.5±34.3 °C
Symbol GHS06
GHS06
Signal Word Danger

 Use of CZC-25146-d3


CZC-25146 Hcl 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-(4-morpholinyl)phenyl]amino}-4-pyrimidinyl)amino]phenyl}methanesulfonamide
Synonym More Synonyms

 CZC-25146-d3 Biological Activity

Description CZC-25146 Hcl 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 C22H26ClFN6O4S
Molecular Weight 525.00
Flash Point 375.5±34.3 °C
LogP 1.50
Vapour Pressure 0.0±2.2 mmHg at 25°C
Index of Refraction 1.655
Storage condition 2-8℃

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301-H319
Precautionary Statements P301 + P310-P305 + P351 + P338
RIDADR UN 2811 6.1 / PGIII

 Synonyms

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