GSK 215

Pricing Availability   Qty
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)
Datasheet
Citations
Reviews
Literature (4)

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.

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.

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

Citations are publications that use Tocris products.

Currently there are no citations for GSK 215. Do you know of a great paper that uses GSK 215 from Tocris? Please let us know.

Reviews 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.


Targeted Protein Degradation Research Product Guide

Targeted Protein Degradation Research Product Guide

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

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

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