DGY-09-192 structure
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Common Name | DGY-09-192 | ||
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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-09-192DGY-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 |
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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. |
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References | 1. Guangyan Du, et al. Angew Chem Int Ed Engl. 2021 Jul 12;60(29):15905-15911. |
Molecular Formula | C49H59Cl2N11O7S |
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Molecular Weight | 1017.041 |