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Description: Potent and selective JAK2/3 Degrader (PROTAC®)
Chemical Name: 4-((4-(1-(3-(Cyanomethyl)-1-(ethylsulfonyl)azetidin-3-yl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-N-(3-(4-(4-(2,6-dioxopiperidin-3-yl)phenyl)piperazin-1-yl)propyl)benzamide
Purity: ≥97% (HPLC)
Biological Activity for SJ 10542
SJ 10542 is a potent and selective JAK2/3 Degrader (PROTAC®) (DC50 values are 11 nM and 14 nM for JAK3 and JAK2, respectively), it uses a phenyl glutarimide (PG) ligand as the cereblon (CRBN) recruiter. SJ 10542 displays high selectivity over GSPT1 and other members of the JAK family. SJ 10542 is active in cytotoxicity assays with PDX models (IC50 values <120 nM).
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Licensing Information
Sold under license from St. Jude Children's Research Hospital
Technical Data for SJ 10542
| M. Wt | 818.96 |
| Formula | C41H46N12O5S |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 2789678-92-6 |
| PubChem ID | 162679331 |
| InChI Key | WBEBZVDAHMXWJN-UHFFFAOYSA-N |
| Smiles | O=C(NC1=O)CCC1C2=CC=C(N3CCN(CCCNC(C4=CC=C(NC5=NC6=C(C=CN6)C(C7=CN(C8(CC#N)CN(S(CC)(=O)=O)C8)N=C7)=N5)C=C4)=O)CC3)C=C2 |
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 SJ 10542
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.95 | 50 |
Preparing Stock Solutions for SJ 10542
The following data is based on the product molecular weight 818.96. 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 | 2.44 mL | 12.21 mL | 24.42 mL |
| 2.5 mM | 0.49 mL | 2.44 mL | 4.88 mL |
| 5 mM | 0.24 mL | 1.22 mL | 2.44 mL |
| 25 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets for SJ 10542
References for SJ 10542
References are publications that support the biological activity of the product.
Alcock et al (2022) Development of potent and selective Janus Kinase 2/3 directing PG-PROTACs. ACS Med.Chem.Lett. 13 475 PMID: 35300081
If you know of a relevant reference for SJ 10542, please let us know.
View Related Products by Target
Keywords: SJ 10542, SJ 10542 supplier, SJ10542, protacs, active, degraders, selective, JAK3, JAK2, kinases, degrades, proteolysis, targeting, chimeras, PROTAC, PROTACS, targeted, protein, degradation, tpd, baricitinib, Active, Degraders, JAK, 7727, Tocris Bioscience
Citations for SJ 10542
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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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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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