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Description: TRIM24 Degrader (PROTAC®)
Chemical Name: (2S,4R)-1-((S)-15-(tert-Butyl)-1-(3-(N-(1,3-dimethyl-2-oxo-6-(3-propoxyphenoxy)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)sulfamoyl)phenyl)-1,13-dioxo-5,8,11-trioxa-2,14-diazahexadecan-16-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Biological Activity
Degrader (PROTAC®) composed of the TRIM24 ligand IACS-9571 conjugated to a VHL ligand. Displays dose- and time-dependent degradation of TRIM24 in cells, with maximum degradation achieved at 5 μM. Degradation phenotypically mirrors genetic deletion of TRIM24. Demonstrates antiproliferative effects in MOLM-13 cells. Cell permeable.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Licensing Information
Sold under license from Dana-Farber Cancer Institute
Technical Data
| M. Wt | 1113.3 |
| Formula | C55H68N8O13S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2170695-14-2 |
| PubChem ID | 131954388 |
| InChI Key | QUQTXFIMYFMULC-OGOZKGDESA-N |
| Smiles | CCCOC1=CC=CC(OC2=C(C=C3N(C(N(C3=C2)C)=O)C)NS(=O)(C4=CC(C(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)O)=O)=O)=O)=CC=C4)=O)=C1 |
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 | 22.27 | 20 | |
| ethanol | 22.27 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 1113.3. 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 |
|---|---|---|---|
| 0.2 mM | 4.49 mL | 22.46 mL | 44.91 mL |
| 1 mM | 0.9 mL | 4.49 mL | 8.98 mL |
| 2 mM | 0.45 mL | 2.25 mL | 4.49 mL |
| 10 mM | 0.09 mL | 0.45 mL | 0.9 mL |
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References
References are publications that support the biological activity of the product.
Gechijian et al (2018) Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands. Nat.Chem.Biol. 14 405 PMID: 29507391
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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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