KL 465

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Description: MAGE-A3 Degrader (PROTAC®)
Chemical Name: (2S,4R)-N-(2-(2-(2-(2-((4-(Furan-2-carbonyl)piperazin-1-yl)methyl)-4-(1H-indazol-4-yl)phenoxy)ethoxy)ethoxy)-4-(4-methylthiazol-5-yl)benzyl)-4-hydroxy-1-((S)-3-methyl-2-(1-oxoisoindolin-2-yl)butanoyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for KL 465

KL 465 is a MAGE-A3 Degrader (PROTAC®) (DC50 = 2 μM; Dmax = 60%). MAGE-A3 degradation with KL 465 decreases cancer cell viability and is VHL dependent.

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

Technical Data for KL 465

M. Wt 1021.2
Formula C56H60N8O9S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 3057446-82-6
InChI Key MQOTXOOWIOCPNH-IYCLWVRSSA-N
Smiles O=C(C1=CC=CO1)N2CCN(CC2)CC3=CC(C4=CC=CC5=C4C=NN5)=CC=C3OCCOCCOC6=CC(C7=C(N=CS7)C)=CC=C6CNC([C@@H]8C[C@H](CN8C([C@H](C(C)C)N9CC%10=C(C9=O)C=CC=C%10)=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 KL 465

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 51.06 50

Preparing Stock Solutions for KL 465

The following data is based on the product molecular weight 1021.2. 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 1.96 mL 9.79 mL 19.58 mL
2.5 mM 0.39 mL 1.96 mL 3.92 mL
5 mM 0.2 mL 0.98 mL 1.96 mL
25 mM 0.04 mL 0.2 mL 0.39 mL

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References for KL 465

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

Li et al (2024) Development of ligands and degraders targeting MAGE-A3. J.Am.Chem.Soc. 146 24884 PMID: 39190582


If you know of a relevant reference for KL 465, please let us know.

View Related Products by Target

Keywords: KL 465, KL 465 supplier, KL465, degrader, degraders, proteolysis, targeting, chimera, PROTAC, degradation, tpd, E3, ligase, VHL, MAGE, A3, Other, Degraders, 8854, Tocris Bioscience

Citations for KL 465

Citations are publications that use Tocris products.

Currently there are no citations for KL 465. Do you know of a great paper that uses KL 465 from Tocris? Please let us know.

Reviews for KL 465

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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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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