GSK 215
Tocris Bioscience, part of Bio-Techne | Catalog # 7818
Potent and selective focal adhesion kinase (FAK) Degrader (PROTAC®)
Key Product Details
Description
Potent and selective focal adhesion kinase (FAK) Degrader (PROTAC®)
Product Description
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.
Product Specifications
Molecular Weight
985.14
Formula
C50H59F3N10O6S
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 98.51 | 100 | |
| Ethanol | 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 all 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 | 0.20 mL | 1.02 mL | 2.03 mL |
| 10 mM | 0.10 mL | 0.51 mL | 1.02 mL |
| 50 mM | 0.02 mL | 0.10 mL | 0.20 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Law Discovery and characterisation of highly cooperative FAK-degrading PROTACs. Angew.Chem.Int.Ed.Engl 2021 PMID: 34416073
Product Specific Notices for GSK 215
For research use only
Loading...
Loading...