WBC100
Based on 1 Customer Validation
WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c-Myc molecule glue degrader. WBC100 is a c-Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c-Myc overexpressing tumors research.
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- Purity: 95.01%
- CAS No.: 2095780-08-6
- 화학식: C25H33NO7
- 분자량:459.53
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
WBC100 selectively kills c-Myc overexpressing cancer cells Mia-paca2, H9, and MOLM-13 cell as well as c-Myc-low normal human cell lines L02, MRC-5 and WI38, the IC50 values are 61 × 10-9, 17 × 10-9, and 16 × 10-9 M for c-Myc overexpressing cancer cells, respectively. Whereas the IC50 values for normal cell lines are 2205 × 10-9, 151 × 10-9, and 570 × 10-9 M, respectively[1]. WBC100 (0-320 nM; 24 hour) decreases c-Myc protein levels in MOLM-13 cells and Mia-paca2 cells in a dose-dependent manner, but has no obvious impact on XPB, Rpb1, and STAT3. Additionally, MG132 can rescue the WBC100-induced decline in c-Myc protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:c-Myc overexpressing cancer cells: Mia-paca2, H9, and MOLM-13 cell c-Myc-low normal human cell lines: L02, MRC-5 and WI38
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Concentration:
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Incubation Time:72 hours
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Result:Preferentially killed c-Myc overexpressing cancer cells.
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Cell Line:Mia-paca2 cells, MOLM-13 cell
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Concentration:0 nM, 20 nM, 40 nM, 80 nM, 160 nM,320 nM
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Incubation Time:24 hours
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Result:Selectively induced degradation of c-Myc protein through E3 ubiquitin ligase CHIP mediated 26S proteasome pathway.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Orthotopic human AML model using NOD/SCID/IL2Rγ-/- (NSG) mice with refractory MOLM-13-luciferase cells with high c-Myc levels
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Dosage:0.1 mg/kg; 0.2 mg/kg; 0.4 mg/kg
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Administration:p.o.; 0.1-0.4 mg/kg; Twice daily; 21 days
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Result:Regresses c-Myc overexpressing refractory acute myeloid leukemia model.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2095780-08-6
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Appearance Solid
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분자량 459.53
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화학식 C25H33NO7
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Color White to off-white
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SMILES
C[C@@]([C@@]1([H])C2)(CCC3=C1COC3=O)[C@]4([C@@]([C@@](O5)([H])[C@@]65C(C)C)([H])O4)[C@@]7([C@@]2([H])O7)[C@@H]6OC([C@H](N)C(C)C)=O
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Synonyms
14-D-Valine-TPL
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (217.61 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 (5.44 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (5.44 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
순도&문서
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.1761 mL | 10.8807 mL | 21.7614 mL | 54.4034 mL |
| 5 mM | 0.4352 mL | 2.1761 mL | 4.3523 mL | 10.8807 mL | |
| 10 mM | 0.2176 mL | 1.0881 mL | 2.1761 mL | 5.4403 mL | |
| 15 mM | 0.1451 mL | 0.7254 mL | 1.4508 mL | 3.6269 mL | |
| 20 mM | 0.1088 mL | 0.5440 mL | 1.0881 mL | 2.7202 mL | |
| 25 mM | 0.0870 mL | 0.4352 mL | 0.8705 mL | 2.1761 mL | |
| 30 mM | 0.0725 mL | 0.3627 mL | 0.7254 mL | 1.8134 mL | |
| 40 mM | 0.0544 mL | 0.2720 mL | 0.5440 mL | 1.3601 mL | |
| 50 mM | 0.0435 mL | 0.2176 mL | 0.4352 mL | 1.0881 mL | |
| 60 mM | 0.0363 mL | 0.1813 mL | 0.3627 mL | 0.9067 mL | |
| 80 mM | 0.0272 mL | 0.1360 mL | 0.2720 mL | 0.6800 mL | |
| 100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5440 mL |
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