GSK 215

Pricing Availability   Qty
Description: Potent and selective focal adhesion kinase (FAK) degrader
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% (HPLC)
Literature (4)

Biological Activity for GSK 215

GSK 215 is a potent and selective focal adhesion kinase (FAK) Degrader (PROTAC®; pDC50 = 8.4, last for 96 h). 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).

Technical Data for GSK 215

M. Wt 985.14
Formula C50H59F3N10O6S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2743427-26-9
PubChem ID 156600270
Smiles FC(F)(F)C(C(NC1=C(C=CC=C1)C(NC)=O)=C2)=CN=C2NC3=C(C=C(N4CCN(CC4)CC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(N=CS7)C)C=C6)C)=O)=O)=O)C=C3)OC

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.

Solubility Data for GSK 215

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 98.51 100
DMSO 98.51 100

Preparing Stock Solutions for GSK 215

The following data is based on the product molecular weight 985.14. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.02 mL 5.08 mL 10.15 mL
5 mM 0.2 mL 1.02 mL 2.03 mL
10 mM 0.1 mL 0.51 mL 1.02 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

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References for GSK 215

References are publications that support the biological activity of the product.

Law et al (2021) Discovery and characterisation of highly cooperative FAK-degrading PROTACs. Angew.Chem.Int.Ed.Engl 60 23327 PMID: 34416073

If you know of a relevant reference for GSK 215, please let us know.

Keywords: GSK 215, GSK 215 supplier, GSK215, potent, selective, Focal, adhesion, kinase, FAK, PROTAC, degraders, degrades, PTK2, Active, Degraders, Adhesion, Kinase, 7818, Tocris Bioscience

Citations for GSK 215

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Literature in this Area

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