DGY-09-192

Chemical Structure : DGY-09-192

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货号: PC-72309Not For Human Use, Lab Use Only.

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.

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生物&药学活性

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.

物理化学性质&存储条件

分子量	1017.041
分子式	C49H59Cl2N11O7S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(2S,4R)-1-((S)-2-(2-(4-(4-((6-(3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-methylureido)pyrimidin-4-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

参考文献

1. Guangyan Du, et al. Angew Chem Int Ed Engl. 2021 Jul 12;60(29):15905-15911.

DGY-09-192

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物理化学性质&存储条件

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DGY-09-192

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