DGY-09-192

Modify Date: 2023-01-20 18:23:33

DGY-09-192 Structure
DGY-09-192 structure
Common Name DGY-09-192
CAS Number 2504949-52-2 Molecular Weight 1017.041
Density N/A Boiling Point N/A
Molecular Formula C49H59Cl2N11O7S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of DGY-09-192


DGY-09-192 is a bivalent degrader (PROTAC) that couples the pan-FGFR inhibitor BGJ398 to a CRL2VHL E3 ligase recruiting ligand,preferentially induces FGFR1/2 degradation while largely sparing FGFR3/4.DGY-09-192 exhibited two-digit nanomolar DC50s for both wildtype FGFR2 and several FGFR2-fusions, resulting in degradation-dependent antiproliferative activity in representative gastric cancer and cholangiocarcinoma cells (IC50=1 nM).DGY-09-192 induced degradation of a clinically relevant FGFR2 fusion protein in xenograft model.

 Names

Name DGY-09-192

 DGY-09-192 Biological Activity

Description DGY-09-192 is a bivalent degrader (PROTAC) that couples the pan-FGFR inhibitor BGJ398 to a CRL2VHL E3 ligase recruiting ligand,preferentially induces FGFR1/2 degradation while largely sparing FGFR3/4.DGY-09-192 exhibited two-digit nanomolar DC50s for both wildtype FGFR2 and several FGFR2-fusions, resulting in degradation-dependent antiproliferative activity in representative gastric cancer and cholangiocarcinoma cells (IC50=1 nM).DGY-09-192 induced degradation of a clinically relevant FGFR2 fusion protein in xenograft model.
References 1. Guangyan Du, et al. Angew Chem Int Ed Engl. 2021 Jul 12;60(29):15905-15911.

 Chemical & Physical Properties

Molecular Formula C49H59Cl2N11O7S
Molecular Weight 1017.041