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Submit ReviewCB-103 New
Description: pan-Notch inhibitor; also inhibits differentiation of mural cells by downregulating Notch pathway.
Alternative Names: Limantrafin
Chemical Name: 6-[4-(1,1-Dimethylethyl)phenoxy]-3-pyridinamine
Purity: ≥98% (HPLC)
Biological Activity for CB-103
CB-103 is a highly specific protein-protein interaction (PPI) inhibitor that interferes with the interaction between the active intracellular domains of Notch receptors (NICD) and the CSL transcription factor complex. In combination with ICI 182,780 (Cat. No. 1047), CB-103 arrests the growth of mouse xenografts from a patient-derived endocrine-resistant model. Also displays potent tumor growth inhibition and delayed tumor relapse when CB-103 was combined with Taxol (Cat. No. 1097). CB-103 inhibits differentiation of mural cells by downregulating Notch pathway.CB-103 is orally bioavailable.
Technical Data for CB-103
| M. Wt | 242.3 |
| Formula | C15H18N2O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 218457-67-1 |
| PubChem ID | 2735289 |
| InChI Key | WHIWGRCYMQLLAO-UHFFFAOYSA-N |
| Smiles | CC(C)(C)C1=CC=C(OC2=CC=C(N)C=N2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CB-103
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 24.23 | 100 | |
| ethanol | 24.23 | 100 |
Preparing Stock Solutions for CB-103
The following data is based on the product molecular weight 242.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.13 mL | 20.64 mL | 41.27 mL |
| 5 mM | 0.83 mL | 4.13 mL | 8.25 mL |
| 10 mM | 0.41 mL | 2.06 mL | 4.13 mL |
| 50 mM | 0.08 mL | 0.41 mL | 0.83 mL |
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Product Datasheets for CB-103
References for CB-103
References are publications that support the biological activity of the product.
Vigolo et al (2023) The efficacy of CB-103, a first-in-class transcriptional Notch inhibitor, in preclinical models of breast cancer. Cancers 15 3957 PMID: 37568775
Gastfriend et al (2024) Notch3 directs differentiation of brain mural cells from human pluripotent stem cell-derived neural crest. Sci.Adv. 10 PMID: 38306433
If you know of a relevant reference for CB-103, please let us know.
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Keywords: CB-103, CB-103 supplier, CB-103, CB103, Limantrafin, protein, interaction, PPI, Notch, pan-Notch, inhibitor, cancer, oncology, orally, bioavailable, tumor, inhibition, Other, Signaling, Differentiation, Products, 9002, Tocris Bioscience
Citations for CB-103
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