dTAGV-1

Tocris Bioscience, part of Bio-Techne | Catalog # 6914

Potent and selective degrader of mutant FKBP12F36V fusion proteins
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Key Product Details

Description

Potent and selective degrader of mutant FKBP12F36V fusion proteins

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Product Description

dTAGV-1 is a 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.

Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use.

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.

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

Product Specifications

Molecular Weight

1361.58

Formula

C68H90N6O14S CF3CO2H

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

CAS Number

2624313-15-9

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.

Solubility

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

Preparing Stock Solutions for dTAGV-1

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 all 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

Calculators

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Background References

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

Product Documents for dTAGV-1

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for dTAGV-1

For research use only

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