Molecular Formula | C15H18N2O |
Molar Mass | 242.32 |
Melting Point | 89-90 |
Solubility | DMSO: 250 mg/mL (1031.69 mM), Need ultrasonic( < 1 mg/ml refers to the product slightly soluble or insoluble) |
Appearance | solid |
Color | Off-white to pale orange |
Storage Condition | 2-8°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Use | CB-103 is a pioneering, orally active notch signaling pathway inhibitor with anti-tumor activity. For details, please refer to the patent literature US9296682B2. |
Hazard Symbols | Xi - Irritant |
Hazard Note | Irritant |
Reference Show more | 1. Freddy Radtke, et al. Inhibitors of notch signalling pathway and use thereof in treatment of cancers. US9296682B2.2. R.Lehal, et al. Development of a novel first-in-class oral inhibitor of the NOTCH pathway.3. Rajwinder Lehal, et al. Non clinical pharmacology, pharmacokinetics and safety profiling of CB-103: A novel first-in-class small molecule inhibitor of the NOTCH pathway. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 4.127 ml | 20.634 ml | 41.268 ml |
5 mM | 0.825 ml | 4.127 ml | 8.254 ml |
10 mM | 0.413 ml | 2.063 ml | 4.127 ml |
5 mM | 0.083 ml | 0.413 ml | 0.825 ml |
biological activity | CB-103 is an orally active inhibitor of the Notch transcriptional activation complex. CB-103 produces a loss-of-Notch phenotype in Drosophila and mice and inhibits the growth of human breast cancer and leukemia xenografts. |
Target | Value |
Cell Line: | RPMI 8402, KOPTK1, PANC1, nRas driven melanoma cells |
Concentration: | 10 μM |
Incubation Time: | 4 days, 6 days |
Result: | Caused a significant reduction in their growth potential. Inhibited growth of GSI/Mab resistant triple negative breast cancer. |
Animal Model: | NSG mice, triple negative breast cancer mouse xenograft model |
Dosage: | 25 mg/kg |
Administration: | Oral administration/Intraperitoneal injection; 2x daily; for 2 weeks |