Edicotinib

Edicotinib is an inhibitor of colony stimulating factor 1 receptor (CSF1R, IC50 = 3.2 nM). It is selective for CSF1R over KIT and FMS-related tyrosine kinase 3 (FLT3, IC50s = 20 and 190 nM, respectively). Edicotinib (0.1-1,000 nM) reduces CSF1-induced phosphorylation of CSF1R and ERK1/2 in N13 microglia. It reduces spinal motor neuron degeneration and increases the latency to fall in the rotarod test in the P301S mouse model of tauopathy. Edicotinib (15 mg/kg) reduces increases in the colonic weight-to-length ratio, as well as decreases colonic infiltration of macrophages, neutrophils, and CD3+ T cells, in an adoptive T cell transfer-induced mouse model of colitis. It also reduces the viability of L-1236 Hodgkin lymphoma cells with an IC50 value of 264 nM.Formal Name: 5-cyano-N-[2-(4,4-dimethyl-1-cyclohexen-1-yl)-6-(tetrahydro-2,2,6,6-tetramethyl-2H-pyran-4-yl)-3-pyridinyl]-1H-imidazole-2-carboxamide. CAS Number: 1142363-52-7. Synonyms: JNJ-40346527, JNJ-527. Molecular Formula: C27H35N5O2. Formula Weight: 461.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 20 mg/ml. lambdamax: 225, 249, 292 nm. SMILES: O=C(C1=NC=C(C#N)N1)NC2=C(C3=CCC(C)(CC3)C)N=C(C4CC(C)(C)OC(C)(C4)C)C=C2. InChi Code: InChI=1S/C27H35N5O2/c1-25(2)11-9-17(10-12-25)22-21(32-24(33)23-29-16-19(15-28)30-23)8-7-20(31-22)18-13-26(3,4)34-27(5,6)14-18/h7-9,16,18H,10-14H2,1-6H3,(H,29,30)(H,32,33). InChi Key: BNVPFDRNGHMRJS-UHFFFAOYSA-N.