| Identification | Back Directory | [Name]
N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide | [CAS]
1191911-26-8 | [Synonyms]
CZC-25146
CHEMBL2397014
LRRK2 Inhibitor II
LRRK2 INHIBITOR II;CZC25146;CZC 25146
N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide
N-(2-((5-fluoro-2-((2-methoxy-4-
morpholinophenyl)amino)pyrimidin-
4-
yl)amino)phenyl)methanesulfonamide
N-[2-[[5-Fluoro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]methanesulfonamide
CZC-25146/N-(2-(2-(2-Methoxy-4-MorpholinophenylaMino)-5-fluoropyriMidin-4-ylaMino)phenyl)MethanesulfonaMide
Methanesulfonamide, N-[2-[[5-fluoro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]- | [Molecular Formula]
C22H25FN6O4S | [MDL Number]
MFCD28160475 | [MOL File]
1191911-26-8.mol | [Molecular Weight]
488.54 |
| Chemical Properties | Back Directory | [Boiling point ]
697.4±65.0 °C(Predicted) | [density ]
1.436±0.06 g/cm3(Predicted) | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
≥24.45 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O | [form ]
solid | [pka]
8.48±0.10(Predicted) | [color ]
Pale purple to purple |
| Hazard Information | Back Directory | [Description]
CZC-25146 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 4.76 nM for the human recombinant kinase). It also inhibits LRRK2G2019S, a mutant linked to neurotoxicity and Parkinson’s disease, with an IC50 value of 6.87 nM. CZC-25146 is selective for LRRK2 over a panel of kinases in HeLa cell lysates, Jurkat/Ramos mixed cell lysates, as well as whole mouse brain extracts (IC50s = >2 μM). It reduces LRRK2G2019S-induced cell injury in rat primary cortical neurons. | [Uses]
CZC-25146 is a compound that acts as an inhibitor of LRRK2, a factor in the expression of Parkinsons’s disease, and is ATP-competitive. | [storage]
Store at -20°C | [References]
[1] ramsden n, perrin j, ren z, et al. chemoproteomics-based design of potent lrrk2-selective lead compounds that attenuate parkinson’s disease-related toxicity in human neurons. acs chemical biology, 2011, 6(10): 1021-1028.
[2] troxler t, greenidge p, zimmermann k, et al. discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of lrrk2. bioorganic & medicinal chemistry letters, 2013, 23(14): 4085-4090. |
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