WEE1 degrader 1
Based on 1 Customer Validation
WEE1 degrader 1 (Compound 10) is a CRBN-dependent molecular glue degrader of WEE1 and casein kinase 1α (CK1α) with sub-2 nM DC50 values for both targets. WEE1 degrader 1 can be used for the research of acute lymphoblastic leukemia, acute monocytic leukemia, acute promyelocytic leukemia, colorectal adenocarcinoma, diffuse large b cell lymphoma.
For research use only. We do not sell to patients.
- Purity: 99.74%
- CAS No.: 3090685-34-7
- Formula: C30H31N5O3
- Molecular Weight:509.60
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
DC50: 1.5 nM (Wee1) [1].
WEE1 degrader 1 (tested concentrations; 5 h) potently induces degradation of both CK1α and WEE1 in Jurkat cells, with sub-2 nM DC50 values and near-complete WEE1 degradation[1].
WEE1 degrader 1 (1 μM; 5 h) potently degrades both WEE1 and CK1α in a broad panel of human hematological and solid tumor cell lines when treated at 1 μM for 5 h[1].
WEE1 degrader 1 (range of concentrations; 72 h) potently inhibits proliferation of multiple human cancer cell lines, with near-complete cell death at 10 μM and EC50 values indicating strong cytotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat, MOLM-14, NB-4, LoVo, SU-DHL-5
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Concentration:1 μM
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Incubation Time:5 h
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Result:Induced potent degradation of both WEE1 and CK1α in Jurkat, MOLM-14, NB-4, LoVo, and SU-DHL-5 cells.
Chemical Information
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CAS No. 3090685-34-7
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Appearance Solid
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Molecular Weight 509.60
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Formula C30H31N5O3
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Color Off-white to light yellow
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SMILES
O=C1N(C2CCC(NC2=O)=O)CC3=C1C=CC(C4=C(N[C@@]56CC(CC(C6)C7)CC7C5)N8C(C=CC=C8)=N4)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (196.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9623 mL | 9.8116 mL | 19.6232 mL | 49.0581 mL |
| 5 mM | 0.3925 mL | 1.9623 mL | 3.9246 mL | 9.8116 mL | |
| 10 mM | 0.1962 mL | 0.9812 mL | 1.9623 mL | 4.9058 mL | |
| 15 mM | 0.1308 mL | 0.6541 mL | 1.3082 mL | 3.2705 mL | |
| 20 mM | 0.0981 mL | 0.4906 mL | 0.9812 mL | 2.4529 mL | |
| 25 mM | 0.0785 mL | 0.3925 mL | 0.7849 mL | 1.9623 mL | |
| 30 mM | 0.0654 mL | 0.3271 mL | 0.6541 mL | 1.6353 mL | |
| 40 mM | 0.0491 mL | 0.2453 mL | 0.4906 mL | 1.2265 mL | |
| 50 mM | 0.0392 mL | 0.1962 mL | 0.3925 mL | 0.9812 mL | |
| 60 mM | 0.0327 mL | 0.1635 mL | 0.3271 mL | 0.8176 mL | |
| 80 mM | 0.0245 mL | 0.1226 mL | 0.2453 mL | 0.6132 mL | |
| 100 mM | 0.0196 mL | 0.0981 mL | 0.1962 mL | 0.4906 mL |
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