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| Targets |
PROTAC BCR-ABL Degrader-1 targets the BCR-ABL fusion protein, a key oncogenic driver in chronic myeloid leukemia (CML) and other hematological malignancies. By binding to BCR-ABL and recruiting an E3 ubiquitin ligase, this PROTAC molecule induces the ubiquitination and subsequent proteasomal degradation of the target protein, thereby suppressing its oncogenic signaling.
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| ln Vitro |
In vitro, PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) induces Bcr-Abl degradation in a ubiquitin-proteasome-dependent manner. This compound also exhibits antiproliferative effects on K562 cells (a CML cell line), indicating its potential for cancer research. The compound is a novel PROTAC designed to selectively degrade the BCR-ABL fusion protein.
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| ln Vivo |
PROTAC BCR-ABL Degrader-1 is designed to induce Bcr-Abl degradation in vivo via the ubiquitin-proteasome pathway. By degrading the oncogenic BCR-ABL fusion protein, it has the potential to inhibit tumor growth in animal models of CML. This compound is useful for investigating its potential as a treatment for CML.
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| Enzyme Assay |
PROTAC BCR-ABL Degrader-1 is a complete PROTAC molecule. A cell-free binding assay is not typical for a full PROTAC. The reported antiproliferative effects are measured in cell-based assays. To confirm binding, researchers could use a TR-FRET assay or SPR with purified BCR-ABL protein to measure the binding affinity of the PROTAC. The compound has a 2-oxoethyl linker.
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| Cell Assay |
K562 cells (human CML cell line) are seeded in 96-well plates in RPMI-1640 medium with 10% FBS. After overnight incubation, cells are treated with varying concentrations of PROTAC BCR-ABL Degrader-1 for 48-72 hours. Cell viability is assessed using the MTT or CellTiter-Glo assay. For Western blot, cells are treated for 6-24 hours, and lysates are probed with anti-BCR-ABL or anti-c-Abl antibodies.
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| Animal Protocol |
A standard in vivo protocol for PROTAC BCR-ABL Degrader-1 would involve a mouse xenograft model. Female NOD/SCID or BALB/c nude mice are injected intravenously with K562 cells. When engraftment is confirmed, mice are randomized and treated intraperitoneally with the PROTAC. Tumor burden is monitored by measuring luciferase activity or human CD45+ cells in blood.
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| ADME/Pharmacokinetics |
PROTAC BCR-ABL Degrader-1 has a molecular weight of 792.84 and the molecular formula C43H40N10O6. It is a solid that can be stored as a powder at -20degC for up to 3 years. In solvent, it is stable for 6 months at -80degC. Specific PK parameters (t½, CL, Vd) have not been reported.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for PROTAC BCR-ABL Degrader-1 are not available. As a research-grade chemical tool, it should be handled with standard laboratory safety precautions, including the use of PPE and a chemical fume hood. Its safety profile has not been established for clinical use.
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| References | |
| Additional Infomation |
PROTAC BCR-ABL Degrader-1 is a research-grade PROTAC and is not approved for clinical use. It is a novel compound that selectively degrades the BCR-ABL protein, making it a valuable tool for investigating its potential as a treatment for chronic myeloid leukemia (CML). It is used in cancer research to study the BCR-ABL signaling pathway and to validate new therapeutic approaches.
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| Molecular Formula |
C43H40N10O6
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| Molecular Weight |
792.84
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| Appearance |
Light yellow to yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2613 mL | 6.3064 mL | 12.6129 mL | |
| 5 mM | 0.2523 mL | 1.2613 mL | 2.5226 mL | |
| 10 mM | 0.1261 mL | 0.6306 mL | 1.2613 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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