1043436-13-0

Basic information

• Product Name: (3S)-3-amino-3-(4-fluorophenyl)-N-methylpropanamide
• Synonyms: (3S)-3-amino-3-(4-fluorophenyl)-N-methylpropanamide
• CAS NO: 1043436-13-0
• Molecular Weight: 196.224
• Mol File: 1043436-13-0.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: (3S)-3-amino-3-(4-fluorophenyl)-N-methylpropanamide(CAS DataBase Reference)
• NIST Chemistry Reference: (3S)-3-amino-3-(4-fluorophenyl)-N-methylpropanamide(1043436-13-0)
• EPA Substance Registry System: (3S)-3-amino-3-(4-fluorophenyl)-N-methylpropanamide(1043436-13-0)

Safety Data

• Hazardous Substances Data: 1043436-13-0(Hazardous Substances Data)

Upstream product

• 479064-88-5 (3S)-3-(4-fluorophenyl)-3-{[(tert-butoxy)carbonyl]amino}propanoic acid 
• 74-89-5 methylamine 

Relevant articles and documents

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands

Androgen receptor (AR) is a validated therapeutic target for the treatment of metastatic castration-resistant prostate cancer (mCRPC). We report herein our design, synthesis, and biological characterization of highly potent small-molecule proteolysis targeting chimera (PROTAC) AR degraders using a potent AR antagonist and E3 ligase ligands with weak binding affinities to VHL protein. Our study resulted in the discovery of 11 (ARD-266), which effectively induces degradation of AR protein in AR-positive (AR+) LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM. ARD-266 is capable of reducing the AR protein level by >95% in these AR+ prostate cancer cell lines and effectively reduces AR-regulated gene expression suppression. For the first time, we demonstrated that an E3 ligand with micromolar binding affinity to its E3 ligase complex can be successfully employed for the design of highly potent and efficient PROTAC degraders and this finding may have a significant implication for the field of PROTAC research.

PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSYNE KINASES

Compounds of formula (I): and their use in the inhibition of Trk activity are described.