NCB-0846

NPC-0846 is an inhibitor of TRAF2- and NCK-interacting kinase (TNIK, IC50 = 21 nM). It is selective for TNIK over a panel of 46 kinases but does inhibit FLT3, JAK3, PDGFRalpha, TrkA, Cdk2/CycA2, and HGK by greater than 80% at 100 nM. NPC-0845 (3 µM) inhibits phosphorylation of transcription factor 4 (TCF4) and autophosphorylation of TNIK in cell-based assays. It inhibits the growth and colony formation of HCT116 colon cancer cells in two-dimensional growth and soft-agar assays, respectively, as well as reduces tumor growth in an HCT116 mouse xenograft model. NPC-0846 (50 and 100 mg/kg) also reduces tumor growth in patient-derived xenograft (PDX) mouse models of colon cancer.Formal Name: cis-4-[[2-(1H-benzimidazol-6-ylamino)-8-quinazolinyl]oxy]-cyclohexanol. CAS Number: 1792999-26-8. Molecular Formula: C21H21N5O2. Formula Weight: 375.4. Purity: >90%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 5 mg/ml. lambdamax: 222, 246, 293, 311 nm. SMILES: O[C@@H](CC1)CC[C@@H]1OC2=CC=CC3=C2N=C(NC4=CC=C(N=CN5)C5=C4)N=C3. InChi Code: InChI=1S/C21H21N5O2/c27-15-5-7-16(8-6-15)28-19-3-1-2-13-11-22-21(26-20(13)19)25-14-4-9-17-18(10-14)24-12-23-17/h1-4,9-12,15-16,27H,5-8H2,(H,23,24)(H,22,25,26)/t15-,16+. InChi Key: FYWRWBSYRGSWIQ-IYBDPMFKSA-N.