BMS-986458
Based on 1 Customer Validation
BMS-986458 is a highly selective, orally active cereblon-based BCL6 PROTAC degrader and antitumor agent. BMS-986458 selectively degrades BCL6 by binding cereblon to the BTB domain of BCL6, thereby regulating the cell cycle, antiproliferative and interferon signaling pathways, and upregulating the expression and distribution of CD20. BMS-986458 modulates the phenotype of follicular helper T cells and reduces circulating tumor DNA levels. The combination of BMS-986458 with CD20xCD3 bispecific antibody also enhances the efficiency of T cell tumor infiltration and expansion. BMS-986458 induces regression of BCL6-positive tumors and prolongs survival, and it is suitable for research related to B-cell non-Hodgkin lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, and relapsed/refractory lymphoma.
(Pink: BCL6 ligand (HY-172740); Blue: Cereblon ligand (HY-W593794); Black: linker (HY-W267161)).
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- Purity: 99.65%
- CAS No.: 3005272-36-3
- 화학식: C32H34ClN9O3
- 분자량:628.12
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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
All PROTACs Isoforms
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Biological Activity
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Cereblon |
BMS-986458 (5 mg/kg; p.o.; BID) monotherapy induces tumor volume reduction and modest CD3+ cell infiltration at the tumor edge, and its combination with Glofitamab demonstrates synergistic antitumor efficacy with enhanced CD3+ cell tumor infiltration in a humanized DLBCL mouse model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:hCRBN NSG mouse Diffuse large B-cell lymphoma (DLBCL) model[3]
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Dosage:5 mg/kg; with Glofitamab (1 μg/mouse IV QW)
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Administration:p.o.; BID
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Result:Induced 59% tumor volume reduction compared to vehicle; showed modest increase in CD3⁺ cells predominantly at the tumor’s edge following 2 weeks of treatment; when combined with glofitamab, achieved 97% tumor volume reduction, 6/8 tumor-free mice, and significant increase in CD3⁺ cell tumor infiltration compared to other groups.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3005272-36-3
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Appearance Solid
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분자량 628.12
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화학식 C32H34ClN9O3
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Color White to off-white
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SMILES
C[C@@H]1CN(CC[C@H]1NC2=CC=C3C(N(N=C3C4CCC(NC4=O)=O)C)=C2)C5=NC=C(C(NC6=CC7=C(N(C(C7)=O)C)C=C6)=N5)Cl
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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 (159.21 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 (3.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
순도&문서
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 1.5921 mL | 7.9603 mL | 15.9205 mL | 39.8013 mL |
| 5 mM | 0.3184 mL | 1.5921 mL | 3.1841 mL | 7.9603 mL | |
| 10 mM | 0.1592 mL | 0.7960 mL | 1.5921 mL | 3.9801 mL | |
| 15 mM | 0.1061 mL | 0.5307 mL | 1.0614 mL | 2.6534 mL | |
| 20 mM | 0.0796 mL | 0.3980 mL | 0.7960 mL | 1.9901 mL | |
| 25 mM | 0.0637 mL | 0.3184 mL | 0.6368 mL | 1.5921 mL | |
| 30 mM | 0.0531 mL | 0.2653 mL | 0.5307 mL | 1.3267 mL | |
| 40 mM | 0.0398 mL | 0.1990 mL | 0.3980 mL | 0.9950 mL | |
| 50 mM | 0.0318 mL | 0.1592 mL | 0.3184 mL | 0.7960 mL | |
| 60 mM | 0.0265 mL | 0.1327 mL | 0.2653 mL | 0.6634 mL | |
| 80 mM | 0.0199 mL | 0.0995 mL | 0.1990 mL | 0.4975 mL | |
| 100 mM | 0.0159 mL | 0.0796 mL | 0.1592 mL | 0.3980 mL |
BMS-986458 Related Classifications
HY-172736 Related Classifications
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