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Submit ReviewSJF 8240 is a c-MET PROTAC® Degrader. Comprises MET inhibitor foretinib joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Degrades c-MET within 6 hours in vitro. Inhibits agonist-driven AKT phosphorylation and GTL16 cell proliferation (IC50 = 66.7 nM). Also degrades exon-14-deleted c-MET in Hs746T cells.
c-MET antibodies validated for Western Blot also available: Catalog # AF276 and MAB5694.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
M. Wt | 1106.25 |
Formula | C58H65F2N7O11S |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 2230821-68-6 |
PubChem ID | 135175904 |
InChI Key | SCUZPTNDZHEHLB-ZWUDBOSPSA-N |
Smiles | COC1=CC2=C(N=CC=C2OC3=C(C=C(C=C3)NC(C4(C(NC5=CC=C(C=C5)F)=O)CC4)=O)F)C=C1OCCCOCCCOCCC(N[C@@H](C(C)(C)C)C(N6C[C@@H](C[C@H]6C(NCC7=CC=C(C8=C(N=CS8)C)C=C7)=O)O)=O)=O |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 55.31 | 50 |
The following data is based on the product molecular weight 1106.25. 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 |
---|---|---|---|
0.5 mM | 1.81 mL | 9.04 mL | 18.08 mL |
2.5 mM | 0.36 mL | 1.81 mL | 3.62 mL |
5 mM | 0.18 mL | 0.9 mL | 1.81 mL |
25 mM | 0.04 mL | 0.18 mL | 0.36 mL |
References are publications that support the biological activity of the product.
Burselem et al (2018) The advantages of targeted protein degradation over inhibition: an RTK case study. Cell Chem.Biol. 25 67 PMID: 29129716
If you know of a relevant reference for SJF 8240, please let us know.
Keywords: SJF 8240, SJF 8240 supplier, SJF8240, cmet, c-MET, degrades, MET, receptor, degraders, protacs, VHL, e3, ligase, targeted, protein, degradation, Receptors, Receptor, Degraders, 7266, Tocris Bioscience
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We use this product to degrade the c-MET from HSAEC1-KT cells prior to infecting them with pathogenic fungi of our interest. We first performed a dose-response assay where we exposed the cells to different concentrations of SJF 8240 overnight in media containing 0.1% DMSO.
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.
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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