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Chemical Structure : GSK215
CAS No.: 2743427-26-9
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $248 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 985.141 | |
| Formula | C50H59F3N10O6S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Law RP, et al. Angew Chem Int Ed Engl. 2021 Oct 18;60(43):23327-23334.
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