SJF 8240

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Description: c-MET PROTAC®; also degrades exon-14-deleted c-MET
Chemical Name: N-(3-Fluoro-4-((7-(3-(3-(3-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-3-oxopropoxy)propoxy)propoxy)-6-methoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews (1)
Literature (2)

Biological Activity for SJF 8240

SJF 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.

Technical Data for SJF 8240

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.

Solubility Data for SJF 8240

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.31 50

Preparing Stock Solutions for SJF 8240

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for SJF 8240

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

Citations for SJF 8240

Citations are publications that use Tocris products.

Currently there are no citations for SJF 8240. Do you know of a great paper that uses SJF 8240 from Tocris? Please let us know.

Reviews for SJF 8240

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SJF 8240.
By Povilas Kavaliauskas on 10/24/2023
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HSAEC1-Kt

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.

review image

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.


TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

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

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
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