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GSK 215

Cat. No. 7818 Submit a Review Datasheet / COA / SDS
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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% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for GSK 215

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 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
InChI Key ZGSWGXNEXAXEGV-XFCHVEHOSA-N
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
Solubility
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.

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Citations for GSK 215

Citations are publications that use Tocris products.

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Literature in this Area

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia