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PROTAC BCR-ABL Degrader-2
Catalog No. T217197 Copy Product Info
🥰Excellent
PROTACBCR-ABLDegrader-2 is a selective Bcr-Abl T315I PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. It demonstrates potent degradation activity with rates of 69.89% at 100 nM and 94.23% at 300 nM concentrations. In vivo, PROTACBCR-ABLDegrader-2 exhibits good plasma exposure, induces significant tumor regression, triggers apoptosis (apoptosis), and maintains a favorable safety profile. This compound is suitable for chronic myelogenous leukemia research.
PROTAC BCR-ABL Degrader-2
Copy Product Info🥰Excellent
Catalog No. T217197
PROTACBCR-ABLDegrader-2 is a selective Bcr-Abl T315I PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. It demonstrates potent degradation activity with rates of 69.89% at 100 nM and 94.23% at 300 nM concentrations. In vivo, PROTACBCR-ABLDegrader-2 exhibits good plasma exposure, induces significant tumor regression, triggers apoptosis (apoptosis), and maintains a favorable safety profile. This compound is suitable for chronic myelogenous leukemia research.
PROTAC BCR-ABL Degrader-2
Cas No. 2703834-25-5
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PROTACBCR-ABLDegrader-2 is a selective Bcr-Abl T315I PROTAC degrader with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. It demonstrates potent degradation activity with rates of 69.89% at 100 nM and 94.23% at 300 nM concentrations. In vivo, PROTACBCR-ABLDegrader-2 exhibits good plasma exposure, induces significant tumor regression, triggers apoptosis (apoptosis), and maintains a favorable safety profile. This compound is suitable for chronic myelogenous leukemia research. |
| In vitro | PROTAC BCR-ABL Degrader-2 (Compound 7o) exhibits an IC50 of 7.7 nM and 4.2 nM in K562 and Ba/F3 Bcr-Abl WT cells, respectively. At concentrations ranging from 0 to 300 nM, it significantly reduces the Bcr-Abl T315I protein level in Ba/F3 Bcr-Abl T315I cells, with a DC50 of 108.7 nM. Additionally, in Bcr-Abl T315I cells, it induces degradation of the Bcr-Abl T315I protein through the CRBN E3 ubiquitination pathway, displaying a "hook effect" over a duration of 0 to 48 hours. |
| In vivo | PROTAC BCR-ABL Degrader-2 (compound 7o) administered as a single intraperitoneal injection at 20 mg/kg maintains a high plasma concentration for up to 48 hours in ICR mice. In a Ba/F3 Bcr-Abl T315I xenograft mouse model, administering PROTAC BCR-ABL Degrader-2 at 10-20 mg/kg every other day for 14 days demonstrates significant antitumor activity and good safety. |
| Molecular Weight | 901.95 |
| Formula | C48H46F3N9O6 |
| Cas No. | 2703834-25-5 |
| Smiles | O=C(NC1=CC=C(C(=C1)C(F)(F)F)CN2CCN(CC2)CCCCCCC(=O)NC3=CC=CC=4C(=O)N(C(=O)C34)C5C(=O)NC(=O)CC5)C6=CC=C(C(C#CC=7C=NC=8NN=CC8C7)=C6)C |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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