2504949-52-2
2504949-52-2 structure
- Name: DGY-09-192
- Chemical Name: DGY-09-192
- CAS Number: 2504949-52-2
- Molecular Formula: C49H59Cl2N11O7S
- Molecular Weight: 1017.041
- Create Date: 2022-07-01 18:02:39
- Modify Date: 2024-09-15 20:08:11
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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.
| Name | DGY-09-192 |
|---|
| 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. |
| Molecular Formula | C49H59Cl2N11O7S |
|---|---|
| Molecular Weight | 1017.041 |