GSK215 | FAK PROTAC | Probechem Biochemicals

Chemical Structure : GSK215

CAS No.: 2743427-26-9

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GSK215 (GSK 215)

货号: PC-72782Not For Human Use, Lab Use Only.

GSK215 is a potent, selective, FAK-degrading Proteolysis Targeting Chimera (PROTAC) based on a binder for the VHL E3 ligase and the known FAK inhibitor VS-4718.

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10 mg	￥3980	In stock
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生物&药学活性

GSK215 is a potent, selective, FAK-degrading Proteolysis Targeting Chimera (PROTAC) based on a binder for the VHL E3 ligase and the known FAK inhibitor VS-4718.
GSK215 showed differentiated in-vitro pharmacology compared to VS-4718.
In mice, a single dose of GSK215 induced rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels (≈96 h) and a marked PK/PD disconnect.

物理化学性质&存储条件

分子量	985.141
分子式	C50H59F3N10O6S
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)-4-hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

参考文献

1. Law RP, et al. Angew Chem Int Ed Engl. 2021 Oct 18;60(43):23327-23334.

GSK215 (GSK 215)

生物&药学活性

物理化学性质&存储条件

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GSK215 (GSK 215)

生物&药学活性

物理化学性质&存储条件

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