For research use only. Not for therapeutic Use.
TNIK-IN-3(Cat No.:I045154)is a potent, orally active inhibitor of the serine/threonine kinase TNIK (TRAF2- and NCK-interacting kinase), exhibiting a strong selectivity with an IC₅₀ of 0.026 µM. It also shows moderate inhibitory activity against Flt4 (IC₅₀ = 0.030 µM), Flt1 (0.191 µM), and DRAK1 (0.411 µM). In colorectal cancer cell lines (HCT‑116 and DLD‑1), TNIK‑IN‑3 displays dose‑dependent antiproliferative effects (IC₅₀ ~4.26 µM and ~8 µM respectively), inhibits colony formation, migration, Wnt target gene expression, and suppresses JNK phosphorylation. In vivo (oral dosing, 100–150 mg/kg twice daily), it significantly reduces tumor growth without overt toxicity.
CAS Number | 2754265-25-1 |
Synonyms | 4-[(4-fluorophenyl)methyl]-8-(1H-pyrrolo[2,3-b]pyridin-5-yl)-2,3-dihydro-1,4-benzoxazepin-5-one |
Molecular Formula | C23H18FN3O2 |
Purity | ≥95% |
IUPAC Name | 4-[(4-fluorophenyl)methyl]-8-(1H-pyrrolo[2,3-b]pyridin-5-yl)-2,3-dihydro-1,4-benzoxazepin-5-one |
InChI | InChI=1S/C23H18FN3O2/c24-19-4-1-15(2-5-19)14-27-9-10-29-21-12-16(3-6-20(21)23(27)28)18-11-17-7-8-25-22(17)26-13-18/h1-8,11-13H,9-10,14H2,(H,25,26) |
InChIKey | UVLOISNMRLZTPF-UHFFFAOYSA-N |
SMILES | C1COC2=C(C=CC(=C2)C3=CN=C4C(=C3)C=CN4)C(=O)N1CC5=CC=C(C=C5)F |
Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |