5-Amino-2-(4-tert-butylphenoxy)pyridine

CB-103 (218457-67-1) is an orally active inhibitor of the Notch signaling activation complex (IC50’s from 0.9 to 3.9 μM in various cell-based assays), the most downstream level of the Notch signaling pathway. It inhibited the growth of Notch-addicted human T cell acute lymphoblastic leukemia cells as well as other cell lines. CB-103 also inhibited the growth of human breast cancer and leukemia xenografts without the intestinal toxicity associated with γ-secretase Notch inhibitors.

Limantrafin (CB-103) is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. Limantrafin has anti-tumor activity[1][2][3][4].

[1] RAJWINDER LEHAL. Pharmacological disruption of the Notch transcription factor complex.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2020: 16292-16301. DOI:10.1073/pnas.1922606117