Synonyms: CB103
Compound class:
Synthetic organic
Comment: CB-103 is a first-in-class, small-molecule, orally active, pan-NOTCH inhibitor that is being investigated for anti-cancer potential [1-2]. It is being developed by Cellestia.
The CAS number provided within the full documentation for the study entitled 'A Phase I/IIA, Multi-Centre, Open-Label, Dose-Escalation Study with Expansion Arms to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of CB-103 Administered Orally in Adult Patients with Advanced or Metastatic Solid Tumours and Haematological Malignancies Characterised by Alterations of the NOTCH Signalling Pathway' (EudraCT protocol 2017-001491-35) allowed us to identify a chemical structure for CB-103, frior to formal name>structure disclosure [2]. Information disclosed in meeting abstract form suggests that CB-103 acts by inhibiting protein-protein interactions that are required to establish assembly of the functional NOTCH transcription complex in the nucleus. By acting at the most downstream point in the NOTCH pathway, CB-103 inhibits NOTCH signalling independently of the mechanisms of NOTCH activation. NOTCH pathway signalling, and the approaches being explored for therapeutic targeting are reviewed by Sorrentino et al., 2019 [3]. |
|
Classification | |
Compound class | Synthetic organic |
IUPAC Name |
6-(4-tert-butylphenoxy)pyridin-3-amine |
Synonyms |
CB103 |
Database Links | |
BindingDB Ligand | 87327 |
CAS Registry No. | 218457-67-1 (source: EudraCT 2017-001491-35) |
ChEMBL Ligand | CHEMBL1420319 |
DrugBank Ligand | DB15279 |
GtoPdb PubChem SID | 387065599 |
PubChem CID | 2735289 |
Search Google for chemical match using the InChIKey | WHIWGRCYMQLLAO-UHFFFAOYSA-N |
Search Google for chemicals with the same backbone | WHIWGRCYMQLLAO |
UniChem Compound Search for chemical match using the InChIKey | WHIWGRCYMQLLAO-UHFFFAOYSA-N |
UniChem Connectivity Search for chemical match using the InChIKey | WHIWGRCYMQLLAO-UHFFFAOYSA-N |