5-AMINO-2-(4-TERT-BUTYLPHENOXY)PYRIDINE
5-AMINO-2-(4-TERT-BUTYLPHENOXY)PYRIDINE Basic information
- Product Name:
- 5-AMINO-2-(4-TERT-BUTYLPHENOXY)PYRIDINE
- Synonyms:
-
- 6-[4-(tert-Butyl)phenoxy]pyridin-3-amine 97%
- 6-[4-(tert-Butyl)phenoxy]pyridin-3-amine97%
- 5-AMINO-2-(4-TERT-BUTYLPHENOXY)PYRIDINE
- 6-[4-(TERT-BUTYL)PHENOXY]PYRIDIN-3-AMINE
- BUTTPARK 96\12-100
- 6-(4-tert-butylphenoxy)-3-pyridinamine
- 3-Pyridinamine, 6-[4-(1,1-dimethylethyl)phenoxy]-
- pathway,CB103,inhibit,Inhibitor,Notch,CB-103,signaling,leukemia,CB 103
- CAS:
- 218457-67-1
- MF:
- C15H18N2O
- MW:
- 242.32
- Mol File:
- 218457-67-1.mol
5-AMINO-2-(4-TERT-BUTYLPHENOXY)PYRIDINE Chemical Properties
- 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)
Safety Information
- Hazard Codes
- Xi
- Hazard Note
- Irritant
- HS Code
- 2933399990
5-AMINO-2-(4-TERT-BUTYLPHENOXY)PYRIDINE Usage And Synthesis
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
[1] RAJWINDER LEHAL. Pharmacological disruption of the Notch transcription factor complex.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2020: 16292-16301. DOI:10.1073/pnas.1922606117
5-AMINO-2-(4-TERT-BUTYLPHENOXY)PYRIDINESupplier
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