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Submit ReviewZNL 02-096
Description: Potent and selective Wee1 Degrader (PROTAC®)
Chemical Name: 4-((3-(4-(4-((2-Allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-3-oxo-2,3-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl)amino)phenyl)piperazin-1-yl)propyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
Purity: ≥98% (HPLC)
Biological Activity for ZNL 02-096
ZNL 02-096 is a potent and selective Wee1 Degrader (PROTAC®) that comprises the Wee1 inhibitor AZD 1775 joined by a linker to the cereblon-binding ligand Pomalidomide (Cat. No. 6302). ZNL 02-096 selectively degrades Wee1 at submicromolar concentrations, while sparing PLK1, an AZD 1775 secondary target. In MOLT-4 cells in vitro, ZNL 02-096 induces degradation of Wee1, accumulation of DNA damage, arrest of the cell cycle in the G2/M phase and apoptosis. The compound shows antiproliferative effects in a panel of 300 cancer cell lines.
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 for ZNL 02-096
| M. Wt | 799.89 |
| Formula | C42H45N11O6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2414418-49-6 |
| PubChem ID | 153555373 |
| InChI Key | LZUDSNUROXNVPH-UHFFFAOYSA-N |
| Smiles | CC(O)(C1=NC(N2N(C(C3=CN=C(N=C23)NC4=CC=C(N5CCN(CC5)CCCNC6=C7C(N(C(C7=CC=C6)=O)C8CCC(NC8=O)=O)=O)C=C4)=O)CC=C)=CC=C1)C |
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 ZNL 02-096
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.99 | 50 |
Preparing Stock Solutions for ZNL 02-096
The following data is based on the product molecular weight 799.89. 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 | 2.5 mL | 12.5 mL | 25 mL |
| 2.5 mM | 0.5 mL | 2.5 mL | 5 mL |
| 5 mM | 0.25 mL | 1.25 mL | 2.5 mL |
| 25 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets for ZNL 02-096
References for ZNL 02-096
References are publications that support the biological activity of the product.
Li et al (2020) Development and characterization of a Wee1 kinase degrader. Cell Chem.Biol. 27 57 PMID: 31735695
If you know of a relevant reference for ZNL 02-096, please let us know.
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Keywords: ZNL 02-096, ZNL 02-096 supplier, ZNL02-096, Wee1, Degrader, PROTAC, PROTACs, AZD, 1775, selective, TPD, targeted, protein, degradation, Active, Degraders, Checkpoint, Kinases, Control, 7240, Tocris Bioscience
Citations for ZNL 02-096
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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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This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
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