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Submit ReviewKL 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.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 51.06 | 50 |
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.
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 |
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.
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 are publications that use Tocris products.
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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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This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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