GSK 215

Tocris Bioscience | Catalog # 7818

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

Key Product Details

Description

Potent and selective focal adhesion kinase (FAK) Degrader (PROTAC®)
View all Active Degraders »

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 for GSK 215

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.

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 0.20 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

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Background References

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

Product Documents for GSK 215

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for GSK 215

For research use only

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