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BMS-986458
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Catalog No. T206353 Copy Product Info
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BMS-986458 is an oral heterobifunctional degrader that targets the Cereblon (CRBN) E3 ubiquitin ligase. By binding to the BTB domain of BCL6, it induces the formation of a ternary complex between BCL6 and CRBN, thereby promoting the ubiquitination and proteasomal degradation of BCL6. BMS-986458 exhibits high selectivity for BCL6 degradation while showing weak degradation activity toward known new CRBN substrates (such as Ikaros, Aiolos, SALL4, and GSPT1), making it a valuable tool for studying BCL6-related tumor signaling pathways and antitumor mechanisms.
Cas No. 3005272-36-3
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $219 | - | In Stock | |
| 5 mg | $496 | - | In Stock | |
| 25 mg | $1,160 | - | In Stock | |
| 100 mg | $2,570 | - | In Stock |
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 | BMS-986458 is an oral heterobifunctional degrader that targets the Cereblon (CRBN) E3 ubiquitin ligase. By binding to the BTB domain of BCL6, it induces the formation of a ternary complex between BCL6 and CRBN, thereby promoting the ubiquitination and proteasomal degradation of BCL6. BMS-986458 exhibits high selectivity for BCL6 degradation while showing weak degradation activity toward known new CRBN substrates (such as Ikaros, Aiolos, SALL4, and GSPT1), making it a valuable tool for studying BCL6-related tumor signaling pathways and antitumor mechanisms. |
| In vivo | BMS-986458 regulates the phenotype of Tfh cells residing in lymphoid tissues in immunocompetent mice without reducing cell viability [1]. BMS-986458 (5 mg/kg; oral; twice daily) induces tumor volume reduction and produces a mild infiltration of CD3+ cells at the tumor margin; in a humanized DLBCL mouse model, its combination with Glofitamab produces synergistic antitumor effects while enhancing the tumor infiltration of CD3+ cells [3]. |
| Molecular Weight | 628.12 |
| Formula | C32H34ClN9O3 |
| Cas No. | 3005272-36-3 |
| Smiles | CN1C=2C(C(=N1)C3C(=O)NC(=O)CC3)=CC=C(N[C@H]4[C@H](C)CN(CC4)C=5N=C(NC=6C=C7C(=CC6)N(C)C(=O)C7)C(Cl)=CN5)C2 |
| Storage | Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (127.36 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
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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.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
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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Related Tags: BMS-986458 chemical structure | BMS-986458 in vivo | BMS-986458 formula | BMS-986458 molecular weight
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