PROTAC BCR-ABL Degrader-1
Based on 1 Customer Validation
PROTAC BCR-ABL Degrader-1 is a PROTAC degrader targeting BCR-ABL, and also selectively inhibits cancer cell proliferation. PROTAC BCR-ABL Degrader-1 induces degradation via the ubiquitin-proteasome system to reduce protein levels. PROTAC BCR-ABL Degrader-1 can be used for research on chronic myeloid leukemia.
(Pink: Bcr-Abl ligand (HY-G0017); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.73%
- CAS No.: 3079412-59-9
- Formula: C43H40N10O6
- Molecular Weight:792.84
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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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Bcr-Abl |
PROTAC BCR-ABL Degrader-1 (Protac 1) (0.1-100 μM; 48 h) potently inhibits the proliferation of K562 cells with an IC50 of 0.62 μM, while it shows low cytotoxicity against normal human NCM460 cells with an IC50 > 100 μM[1].
PROTAC BCR-ABL Degrader-1 (1-20 μM; 48 h) reduces the protein levels of BCR-ABL and c-ABL in K562 cells in a dose-dependent manner[1].
PROTAC BCR-ABL Degrader-1 (10 μM; 4-48 h) reduces the protein levels of BCR-ABL and c-ABL in K562 cells in a time-dependent manner[1].
PROTAC BCR-ABL Degrader-1 (10 μM; 48 h following 1 h pre-incubation with proteasome inhibitors) induces the degradation of BCR-ABL in K562 cells in a ubiquitin-proteasome-dependent manner, which is supported by the finding that the proteasome inhibitors MG132 (HY-13259) and Bortezomib (HY-10227) attenuate this degradation effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 chronic myeloid leukemia cells
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Concentration:0.1, 1, 10, 50, 100 μM
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Incubation Time:48 h
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Result:Exhibited significant antiproliferative activity against K562 cells, with an IC50 of 0.62 μM.
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Cell Line:K562 chronic myeloid leukemia cells
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Concentration:1, 5, 10, 20 μM
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Incubation Time:48 h
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Result:Reduced BCR-ABL protein levels in a dose-dependent manner; concentrations of 5-20 μM significantly decreased BCR-ABL levels, with near-complete degradation at 20 μM.
Significantly reduced c-ABL protein levels at concentrations above 5 μM, with the most pronounced effect at 20 μM.
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Cell Line:K562 chronic myeloid leukemia cells
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Concentration:10 μM
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Incubation Time:4, 24, 48 h
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Result:Reduced BCR-ABL protein levels in a time-dependent manner; BCR-ABL levels were reduced after 24 h of treatment, and near-complete degradation was observed after 48 h.
Decreased c-ABL protein levels over time, with significant reduction seen at 24 and 48 h.
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Cell Line:K562 chronic myeloid leukemia cells
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Concentration:10 μM
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Incubation Time:48 h (following 1 h pre-incubation with proteasome inhibitors)
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Result:Alone significantly reduced BCR-ABL protein levels, but pre-treatment with MG132 or Bortezomib attenuated this degradation activity.
Pre-treatment with Thalidomide did not completely block BCR-ABL degradation.
Chemical Information
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CAS No. 3079412-59-9
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Appearance Solid
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Molecular Weight 792.84
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Formula C43H40N10O6
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Color Light yellow to yellow
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SMILES
CC(C=CC(NC(C1=CC=C(CN2CCN(CC(NC3=CC=CC4=C3C(N(C5C(NC(CC5)=O)=O)C4=O)=O)=O)CC2)C=C1)=O)=C6)=C6NC7=NC=CC(C8=CC=CN=C8)=N7
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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 (126.13 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 (3.15 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.
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 (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 1.2613 mL | 6.3064 mL | 12.6129 mL | 31.5322 mL |
| 5 mM | 0.2523 mL | 1.2613 mL | 2.5226 mL | 6.3064 mL | |
| 10 mM | 0.1261 mL | 0.6306 mL | 1.2613 mL | 3.1532 mL | |
| 15 mM | 0.0841 mL | 0.4204 mL | 0.8409 mL | 2.1021 mL | |
| 20 mM | 0.0631 mL | 0.3153 mL | 0.6306 mL | 1.5766 mL | |
| 25 mM | 0.0505 mL | 0.2523 mL | 0.5045 mL | 1.2613 mL | |
| 30 mM | 0.0420 mL | 0.2102 mL | 0.4204 mL | 1.0511 mL | |
| 40 mM | 0.0315 mL | 0.1577 mL | 0.3153 mL | 0.7883 mL | |
| 50 mM | 0.0252 mL | 0.1261 mL | 0.2523 mL | 0.6306 mL | |
| 60 mM | 0.0210 mL | 0.1051 mL | 0.2102 mL | 0.5255 mL | |
| 80 mM | 0.0158 mL | 0.0788 mL | 0.1577 mL | 0.3942 mL | |
| 100 mM | 0.0126 mL | 0.0631 mL | 0.1261 mL | 0.3153 mL |
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