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GSK 215

Catalog #: 7818 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7818/5
GSK 215 | CAS No. 2743427-26-9 | Active Degraders
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Description: Potent and selective focal adhesion kinase (FAK) Degrader (PROTAC®)

Chemical Name: (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

Purity: ≥98%

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Biological Activity

GSK 215 is a potent and selective focal adhesion kinase (FAK) Degrader (PROTAC®; DC50 = 1.3 nM, Dmax = 90%). Comprises the FAK inhibitor, PND 1186 (Cat. No. 6891), joined by a linker to a VHL E3 ligase ligand. Kinome binding (KinoBead profiling) shows GSK 215 (at 10 nM) has high selectivity for the FAK kinase domain. GSK 215 inhibits cell proliferation in MCF-7 and A549 cells and suppresses A549 cell motility in a wound scratch model system. In CD1 mice, GSK 215 injection induces rapid and profound degradation of FAK in liver (Dmax = 85% at 18h).

PROTAC� is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data

M.Wt:
985.14
Formula:
C50H59F3N10O6S
Solubility:
Soluble to 100 mM in ethanol and to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2743427-26-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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