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VHF 543, amine

Cat. No. 8075 Submit a Review Datasheet / COA / SDS
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Description: DCAF1 WD40 ligand with terminal amine for onward chemistry
Chemical Name: 1-(4-(4-((2-Aminoethyl)amino)-2-(1-(4-chlorophenyl)cyclohexyl)quinazolin-7-yl)piperazin-1-yl)ethan-1-one
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for VHF 543, amine

VHF 543, amine is a potent ligand for the WD40 repeat domain (WDR) of DCAF1 (Kd = 31 nM measured by surface plasmon resonance). VHF 543, amine is supplied with a primary amine functional handle, for ready conjugation to a linker/target protein ligand.

Please contact us for SD files of our available Degrader Building Blocks.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data for VHF 543, amine

M. Wt 507.08
Formula C28H35ClN6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 3053860-67-3
PubChem ID 168069227
InChI Key GGEKTDCCHNVLNE-UHFFFAOYSA-N
Smiles NCCNC1=NC(C2(C3=CC=C(C=C3)Cl)CCCCC2)=NC4=CC(N5CCN(CC5)C(C)=O)=CC=C41

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 VHF 543, amine

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.14 20

Preparing Stock Solutions for VHF 543, amine

The following data is based on the product molecular weight 507.08. 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
0.2 mM 9.86 mL 49.3 mL 98.6 mL
1 mM 1.97 mL 9.86 mL 19.72 mL
2 mM 0.99 mL 4.93 mL 9.86 mL
10 mM 0.2 mL 0.99 mL 1.97 mL

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Product Datasheets for VHF 543, amine

Certificate of Analysis / Product Datasheet
Safety Datasheet

References for VHF 543, amine

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

Vulpetti et al (2023) Discovery of new binders for DCAF1, an emerging ligase target in the targeted protein degradation field. ACS Med.Chem.Lett. 14 949 PMID: 37465299

If you know of a relevant reference for VHF 543, amine, please let us know.

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Citations for VHF 543, amine

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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!

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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