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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)
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 |
| 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.
| 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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Product Datasheets for GSK 215
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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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
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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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