dTAGV-1

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Cat.No. 6914 - dTAGV-1 | C68H90N6O14S CF3CO2H
Description: Potent and selective degrader of mutant FKBP12F36V fusion proteins
Chemical Name: (R)-3-(3,4-Dimethoxyphenyl)-1-(2-(2-((7-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-7-oxoheptyl)amino)-2-oxoethoxy)phenyl)propyl (S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate trifluoroacetate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity

Degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS/FLI-expressing Ewing sarcoma cells.

Negative control dTAGV-1-NEG (Cat. No. 6915) also available.

FKBP12F36V can be expressed as a fusion with a target protein of interest using genome engineering techniques, via transgene expression or CRISPR-mediated locus-specific knock-in. Custom knock-in cell lines for the dTAG and aTAG platforms are available from our sister brand R&D Systems. Email TPD@bio-techne.com to enquire.

Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Technical Data

M. Wt 1361.58
Formula C68H90N6O14S CF3CO2H
Storage Store at -20°C
Purity ≥98% (HPLC)
InChI Key KSEWNBIDXKMTNT-LNVAYBNASA-N
Smiles C[C@H](NC([C@@H]1C[C@@H](O)CN1C([C@@H](NC(CCCCCCNC(COC2=CC=CC=C2[C@H](OC([C@@H]3CCCCN3C([C@@H](CC)C4=CC(OC)=C(OC)C(OC)=C4)=O)=O)CCC5=CC(OC)=C(OC)C=C5)=O)=O)C(C)(C)C)=O)=O)C6=CC=C(C=C6)C7=C(N=CS7)C.OC(C(F)(F)F)=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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 136.16 100

Preparing Stock Solutions

The following data is based on the product molecular weight 1361.58. 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 0.73 mL 3.67 mL 7.34 mL
5 mM 0.15 mL 0.73 mL 1.47 mL
10 mM 0.07 mL 0.37 mL 0.73 mL
50 mM 0.01 mL 0.07 mL 0.15 mL

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References

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

Nabet et al (2020) Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nat.Commun. 11 4687 PMID: 32948771


If you know of a relevant reference for dTAGV-1, please let us know.

Keywords: dTAGV-1, dTAGV-1 supplier, 2451573-86-5, dTAGVHL1, degraders, degrades, targeted, protein, degradation, FKBP12F36V, fusion, mutant, PROTAC, VHL, von, Hippel, Lindau, TPD, TAG, Degradation, Platform, 6914, Tocris Bioscience

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Targeted Protein Degradation

Targeted Protein Degradation Research Product Guide

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Targeted Protein Degradation

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