GSK 215

Name: GSK 215
Brand: Tocris Bioscience
SKU: 7818

Tocris Bioscience, part of Bio-Techne | Catalog # 7818

COA / SDS

Potent and selective focal adhesion kinase (FAK) Degrader (PROTAC®)

Key Product Details

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)
Molecular Weight:	985.14

View Full Technical Details for GSK 215

Technical Data
Citations

Biological Activity for GSK 215

GSK 215 is a potent and selective focal adhesion kinase (FAK) Degrader (PROTAC^®; DC₅₀ = 1.3 nM, D_max = 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 (D_max = 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 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	0.20 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

References for GSK 215

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