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CB-103 is a first-in-class, orally active inhibitor of the Notch transcription activation complex. 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. CB-103 exhibits anti-tumor efficacy in GSI resistant T-ALL cell lines. CB-103 produces Notch loss-of-function phenotypes in flies and mice and inhibits the growth of human breast cancer and leukemia xenografts, notably without causing the dose-limiting intestinal toxicity associated with other Notch inhibitors.
In vivo, CB-103 (25 mg/kg; i.p./p.o.; 2x daily; for 2 weeks) inhibits growth of GSI/Mab resistant triple negative breast cancer.
| Molecular Weight | 242.32 |
| Formula | C15H18N2O |
| CAS Number | 218457-67-1 |
| Solubility (25°C) | DMSO ≥ 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Doriano Fabbro, et al. Chimia (Aarau). Notch Inhibition in Cancer: Challenges and Opportunities
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