CZC-25146

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.Formal Name: N-[2-[[5-fluoro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-methanesulfonamide. CAS Number: 1191911-26-8. Molecular Formula: C22H25FN6O4S. Formula Weight: 488.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 10 mg/ml. lambdamax: 281 nm. SMILES: COC1=CC(N2CCOCC2)=CC=C1NC3=NC=C(F)C(NC4=CC=CC=C4NS(C)(=O)=O)=N3. InChi Code: InChI=1S/C22H25FN6O4S/c1-32-20-13-15(29-9-11-33-12-10-29)7-8-19(20)26-22-24-14-16(23)21(27-22)25-17-5-3-4-6-18(17)28-34(2,30)31/h3-8,13-14,28H,9-12H2,1-2H3,(H2,24,25,26,27). InChi Key: XXHHOTZUJIXPJX-UHFFFAOYSA-N.