| Identification | More | [Name]
5-AMINO-2-(4-TERT-BUTYLPHENOXY)PYRIDINE | [CAS]
218457-67-1 | [Synonyms]
5-AMINO-2-(4-TERT-BUTYLPHENOXY)PYRIDINE
6-[4-(TERT-BUTYL)PHENOXY]PYRIDIN-3-AMINE
BUTTPARK 96\12-100 | [Molecular Formula]
C15H18N2O | [MDL Number]
MFCD00052647 | [Molecular Weight]
242.32 | [MOL File]
218457-67-1.mol |
| Chemical Properties | Back Directory | [Melting point ]
89-90 | [storage temp. ]
2-8°C | [solubility ]
Soluble in DMSO (>30 mg/ml) | [form ]
solid | [color ]
Off-white to pale orange | [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. | [CAS DataBase Reference]
218457-67-1(CAS DataBase Reference) |
| Hazard Information | Back Directory | [Description]
CB-103 (218457-67-1) is an orally active inhibitor of the Notch signaling activation complex (IC50’s from 0.9 to 3.9 μM in various cell-based assays), the most downstream level of the Notch signaling pathway. It inhibited the growth of Notch-addicted human T cell acute lymphoblastic leukemia cells as well as other cell lines.? CB-103 also inhibited the growth of human breast cancer and leukemia xenografts without the intestinal toxicity associated with γ-secretase Notch inhibitors. | [Uses]
Limantrafin (CB-103) is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. Limantrafin has anti-tumor activity[1][2][3][4]. | [in vivo]
Limantrafin inhibits NOTCH dependent cellular processes in mice[2].
Limantrafin blocks in vivo growth of PDX models of T-ALL[2].
Limantrafin (25 mg/kg; i.p./p.o.; 2x daily; for 2 weeks) inhibits growth of GSI/Mab resistant triple negative breast cancer[3].
Limantrafin exhibits anti-tumor activity in xenograft models of human T-ALL and mouse mammary tumors[3].
| Animal Model: | NSG mice, triple negative breast cancer mouse xenograft model[3] | | Dosage: | 25 mg/kg | | Administration: | Oral administration/Intraperitoneal injection; 2x daily; for 2 weeks | | Result: | Inhibited growth of GSI/Mab resistant triple negative breast cancer. |
| [References]
Lehal et al. (2020), Pharmacological disruption of the Notch transcription factor complex; Proc. Natl. Acad. Sci. USA, 117 16292 |
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