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Chemical Structure : CB-103
CAS No.: 218457-67-1
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).
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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.
| M.Wt | 242.322 | |
| Formula | C15H18N2O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
100 mM in DMSO (24 mg/mL) |
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| Chemical Name/SMILES |
6-(4-(tert-butyl)phenoxy)pyridine-3-amine |
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1. Lehal R, et al. Proc Natl Acad Sci U S A. 2020 Jul 14;117(28):16292-16301.
2. Lue JK, et al. Ann Lymphoma. 2020 Sep 30;4:7.
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