aTAG 4531

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Description: Degrader of MTH1 fusion proteins for use within the aTAG system
Alternative Names: CFT 4531
Chemical Name: N-Cyclopropyl-6-(4-((4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)methyl)-1H-1,2,3-triazol-1-yl)butyl)carbamoyl)-3-fluorophenyl)-7-fluoro-4-(phenylamino)quinoline-3-carboxamide
Purity: ≥98% (HPLC)
Protocols (1)
Literature (3)

Biological Activity for aTAG 4531

aTAG 4531 is a degrader of MTH1 fusion proteins for use within the aTAG system. Comprises a ligand selective for MTH1, a linker and the cereblon-binding ligand Thalidomide (Cat. No. 0652). Induces highly potent and selective degradation of fusion proteins after a 4 h incubation (DC50 = 0.34 nM; Dmax = 93.14%). Cell-permeable. Suitable for in vitro and in vivo applications.

Mouse DMPK properties are provided in the supplementary file (see below).

MTH1 can be expressed as a fusion with a target protein of interest using genome engineering techniques via CRISPR-mediated locus-specific knock-in. See protocol for more information.

Custom knock-in cell lines for the dTAG and aTAG platforms are available from Bio-Techne.

Licensing Information

Sold under license from C4 Therapeutics

Supplementary Information for aTAG 4531

Mouse DMPK properties are provided in the accompanying supplementary file.

Technical Data for aTAG 4531

M. Wt 867.85
Formula C46H39F2N9O7
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2412985-00-1
Smiles O=C(NC1CC1)C2=C(C3=C(N=C2)C=C(F)C(C4=CC(F)=C(C=C4)C(NCCCCN5N=NC(COC6=C(C7=CC=C6)C(N(C7=O)C8C(NC(CC8)=O)=O)=O)=C5)=O)=C3)NC9=CC=CC=C9

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 aTAG 4531

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 86.78 100

Preparing Stock Solutions for aTAG 4531

The following data is based on the product molecular weight 867.85. 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 1.15 mL 5.76 mL 11.52 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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Product Datasheets for aTAG 4531

Certificate of Analysis / Product Datasheet
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References for aTAG 4531

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

If you know of a relevant reference for aTAG 4531, please let us know.

Keywords: aTAG 4531, aTAG 4531 supplier, aTAG4531, CFT4531, atag, Achilles, heel, degraders, degradation, MTH1, fusion, protein, PROTAC, proteolysis, targeting, chimeras, targeted, TPD, CFT, 4531, TAG, Degradation, Platform, 6971, Tocris Bioscience

Citations for aTAG 4531

Citations are publications that use Tocris products.

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Protocols for aTAG 4531

The following protocol features additional information for the use of aTAG 4531 (Cat. No. 6971).

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
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

Validating Targets for TPD Using dTAG Poster

Validating Targets for TPD Using dTAG Poster

The dTAG platform offers a generalizable strategy to degrade, in principle, any intracellular protein of interest (POI) and is a useful strategy for exploration and validation of targets. This poster presents a workflow solution for target validation, from custom TAG knock-in cell-lines for your POI, different dTAG Degraders to knockdown you POI, to automated assays for protein degradation using Simple WesternTM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.