HEMTAC WEE1 degrader-1
Based on 1 Customer Validation
HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.78%
- CAS No.: 3002417-64-0
- Formula: C57H71N15O6
- Molecular Weight:1062.27
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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HSP90 16.76 nM (IC50) |
Hsp90TACs |
HEMTAC WEE1 degrader-1 (Compound 9c) (72 h) inhibits the proliferation activity of MV-4-11 cells (IC50: 8.08 nM) and primary AML cells (IC50: 4.77 nM)[1].
HEMTAC WEE1 degrader-1 (0.01-10 μM, 12 h) degrades WEE1 protein in MV-4-11 cells and has a minor effect on AKT protein, indicating that this effect is independent of HSP90 inhibition[1].
HEMTAC WEE1 degrader-1 (0.1-10 μM, 12 h) promotes the expression of WEE1 mRNA in MV-4-11 cells in a concentration-dependent manner[1].
HEMTAC WEE1 degrader-1 (3-30 nM, 72 h) induces cell cycle arrest at the G2/M phase of MV-4-11 cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11 cells
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Concentration:0.01 μM, 0.1 μM, 1 μM and 10 μM
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Incubation Time:12 h
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Result:Down-regulated the expression of WEE1 protein.
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Cell Line:MV-4-11 cells
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Concentration:0.1 μM, 1 μM and 10 μM
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Incubation Time:12 h
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Result:Up-regulated the expression of WEE1 mRNA.
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Cell Line:MV-4-11 cells
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Concentration:3 nM, 10 nM and 30 nM
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Incubation Time:72 h
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Result:Induced a large accumulation of cells in the G2/M phase.
HEMTAC WEE1 degrader-1 (10 mg/kg, i.v., once every day for 3 d) has minimal myelosuppressive toxicity in healthy mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AML patient-derived xenograft (PDX) model, Female NOD/SCID mice (6-9 weeks old)[1]
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Dosage:3 mg/kg
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Administration:Intravenous injection (i.v.), once every day for 4 weeks
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Result:Reduced the percentage of huCD45-positive cells in the bone marrow (>75%).
Inhibited splenomegaly.
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Animal Model:Healthy male BALA/C mice (20-22 g)[1]
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Dosage:10 mg/kg
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Administration:Intravenous injection (i.v.), once every day for 3 d
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Result:Had minimal effect on platelets, leukocytes and neutrophils
Chemical Information
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CAS No. 3002417-64-0
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Appearance Solid
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Molecular Weight 1062.27
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Formula C57H71N15O6
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Color Light yellow to yellow
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SMILES
O=C(C1=NN=C(C2=CC(C(C)C)=C(O)C=C2O)N1C3=CC=C(CN4CCN(CC(NCCCCN5CCN(C6=CC=C(NC7=NC=C8C(N(C9=NC(C(C)(O)C)=CC=C9)N(CC=C)C8=O)=N7)C=C6)CC5)=O)CC4)C=C3)NCC
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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 (94.14 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 (2.35 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.
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 (275 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 |
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| DMSO | 1 mM | 0.9414 mL | 4.7069 mL | 9.4138 mL | 23.5345 mL |
| 5 mM | 0.1883 mL | 0.9414 mL | 1.8828 mL | 4.7069 mL | |
| 10 mM | 0.0941 mL | 0.4707 mL | 0.9414 mL | 2.3535 mL | |
| 15 mM | 0.0628 mL | 0.3138 mL | 0.6276 mL | 1.5690 mL | |
| 20 mM | 0.0471 mL | 0.2353 mL | 0.4707 mL | 1.1767 mL | |
| 25 mM | 0.0377 mL | 0.1883 mL | 0.3766 mL | 0.9414 mL | |
| 30 mM | 0.0314 mL | 0.1569 mL | 0.3138 mL | 0.7845 mL | |
| 40 mM | 0.0235 mL | 0.1177 mL | 0.2353 mL | 0.5884 mL | |
| 50 mM | 0.0188 mL | 0.0941 mL | 0.1883 mL | 0.4707 mL | |
| 60 mM | 0.0157 mL | 0.0784 mL | 0.1569 mL | 0.3922 mL | |
| 80 mM | 0.0118 mL | 0.0588 mL | 0.1177 mL | 0.2942 mL |
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