Catalog No.: PC-38257Not For Human Use, Lab Use Only.
CB-103 (CB103) is an orally active small-molecule inhibitor of the Notch transcription activation complex, inhibits both ligand-dependent and ligand-independent Notch activation in cell-based assays (IC50=0.9-3.9 uM).
CB-103 (CB103) is an orally active small-molecule inhibitor of the Notch transcription activation complex, inhibits both ligand-dependent and ligand-independent Notch activation in cell-based assays (IC50=0.9-3.9 uM).
CB-103 does not inhibit Wnt or Hedgehog signaling using reporter assays.
CB-103 inhibits Notch signaling in primary human T cell acute lymphoblastic leukemia and other Notch-dependent human tumor cell lines, and concomitantly induces cell cycle arrest and apoptosis, thereby impairing proliferation, including in GSI-resistant human tumor cell lines with chromosomal translocations and rearrangements in Notch genes.
CB-103 produces Notch loss-of-function phenotypes in flies and mice. CB-103 inhibits the growth of human breast cancer and leukemia xenografts, notably without causing the dose-limiting intestinal toxicity associated with other Notch inhibitors.
Physicochemical Properties
M.Wt
242.322
Formula
C15H18N2O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
100 mM in DMSO (24 mg/mL)
Chemical Name/SMILES
6-(4-(tert-butyl)phenoxy)pyridine-3-amine
References
1. Lehal R, et al. Proc Natl Acad Sci U S A. 2020 Jul 14;117(28):16292-16301.
