PROTAC BCL6 Degrader-2
Based on 1 Customer Validation
PROTAC BCL6 Degrader-2 is an orally active, selective BCL6 PROTAC degrader (DC50: 0.45 nM in HEK293T cells). PROTAC BCL6 Degrader-2 promotes ubiquitination and degradation of BCL6. It exhibits anticancer activity against BCL6-dependent diffuse large B-cell lymphoma. PROTAC BCL6 Degrader-2 can be used for the research of diffuse large B-cell lymphoma.
(Pink: BCL6 ligand (HY-178804); Blue: Cereblon ligand (HY-W087383); Black: linker).
For research use only. We do not sell to patients.
- Purity : 99.70%
- Formula: C46H52ClN11O8
- Molecular Weight:922.43
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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
Description
IC50 & Target
[1]|
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | DC50 |
0.45 nM
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BCL6 degradation in HEK293T cells stably expressing BCL6-GFP evaluated using a real-time imaging degradation system after 24 h incubation.
BCL6 degradation in HEK293T cells stably expressing BCL6-GFP evaluated using a real-time imaging degradation system after 24 h incubation.
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41025654 |
| OCI-Ly1 | IC50 |
12.78 nM
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Cell growth inhibition against OCI-LY1 diffuse large B-cell lymphoma cells assessed as reduction in cell viability incubated for 7 days by CCK8 assay.
Cell growth inhibition against OCI-LY1 diffuse large B-cell lymphoma cells assessed as reduction in cell viability incubated for 7 days by CCK8 assay.
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41025654 |
| HT | IC50 |
36.30 nM
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Cell growth inhibition against HT BCL6-dependent diffuse large B-cell lymphoma cells assessed as reduction in cell viability incubated for 7 days by CCK8 assay.
Cell growth inhibition against HT BCL6-dependent diffuse large B-cell lymphoma cells assessed as reduction in cell viability incubated for 7 days by CCK8 assay.
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41025654 |
| OCI-Ly10 | IC50 |
835.33 nM
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Cell growth inhibition against OCI-LY10 BCL6-dependent diffuse large B-cell lymphoma cells assessed as reduction in cell viability incubated for 7 days by CCK8 assay.
Cell growth inhibition against OCI-LY10 BCL6-dependent diffuse large B-cell lymphoma cells assessed as reduction in cell viability incubated for 7 days by CCK8 assay.
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41025654 |
| Toledo | IC50 |
>10000 nM
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Cell growth inhibition against Toledo BCL6-independent diffuse large B-cell lymphoma cells assessed as reduction in cell viability incubated for 7 days by CCK8 assay.
Cell growth inhibition against Toledo BCL6-independent diffuse large B-cell lymphoma cells assessed as reduction in cell viability incubated for 7 days by CCK8 assay.
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41025654 |
| OCI-Ly1 | DC50 |
0.034 nM
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BCL6 degradation in OCI-LY1 diffuse large B-cell lymphoma cells analyzed via Western blotting after 24 h incubation.
BCL6 degradation in OCI-LY1 diffuse large B-cell lymphoma cells analyzed via Western blotting after 24 h incubation.
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41025654 |
| HT | DC50 |
0.096 nM
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BCL6 degradation in HT diffuse large B-cell lymphoma cells analyzed via Western blotting after 24 h incubation.
BCL6 degradation in HT diffuse large B-cell lymphoma cells analyzed via Western blotting after 24 h incubation.
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41025654 |
In Vitro
PROTAC BCL6 Degrader-2 (Compound A19) (0.001-100 nM; 24 h) potently degrades BCL6 in HEK293T cells stably expressing BCL6-GFP, with a DC50 of 0.45 nM and a maximum degradation rate of up to 94.60% at a concentration of 100 nM[1].
PROTAC BCL6 Degrader-2 (0.001-100 nM; 0-24 h) potently and rapidly degrades BCL6 in OCI-LY1 diffuse large B-cell lymphoma (DLBCL) cells, with a DC50 of 0.034 nM, a maximum degradation rate of >99% at 24 h, and complete degradation achieved within 1 h at a concentration of 40 nM[1].
PROTAC BCL6 Degrader-2 (10 nM; 6 h) selectively degrades BCL6 in OCI-LY1 diffuse large B-cell lymphoma (DLBCL) cells, with no effect on the novel CRBN substrates IKZF1, IKZF2, IKZF3 or GSPT1[1].
PROTAC BCL6 Degrader-2 (7 days) potently inhibits the proliferation of OCI-LY1 diffuse large B-cell lymphoma (DLBCL) cells, with an IC50 value of 12.78 nM[1].
PROTAC BCL6 Degrader-2 (7 days) inhibits the growth of BCL6-dependent HT, SU-DHL4 and OCI-LY10 diffuse large B-cell lymphoma (DLBCL) cells, with corresponding IC50 values of 36.30 nM, 500.00 nM and 835.33 nM, but shows no activity in BCL6-independent Toledo DLBCL cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OCI-LY1 diffuse large B-cell lymphoma (DLBCL) cells
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Concentration:Multiple concentrations
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Incubation Time:7 days
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Result:Inhibited OCI-LY1 cell growth with an IC50 of 12.78 nM.
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Cell Line:HT, SU-DHL4, OCI-LY10 BCL6-dependent DLBCL cells; Toledo BCL6-independent DLBCL cells
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Concentration:Multiple concentrations
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Incubation Time:7 days
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Result:Inhibited cell growth with IC50 values of 36.30 nM in HT cells, 500.00 nM in SU-DHL4 cells.
Showed no activity (IC50 > 10000 nM) in Toledo cells.
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Cell Line:OCI-LY1 DLBCL cells
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Concentration:0.001-100 nM (24 h); 40 nM (time-course)
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Incubation Time:24 h (concentration-dependent); 0-24 h (time-course at 40 nM)
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Result:Induced concentration-dependent BCL6 degradation with a DC50 of 0.034 nM and a Dmax of >99% at 24 h.
Achieved complete BCL6 degradation within 1 h at 40 nM.
Parmacokinetics
| Species | Dose | Route | Tmax | T1/2 | Cmax | AUC0-t | AUC0-∞ |
|---|---|---|---|---|---|---|---|
| Mice[1] | 30 mg/kg | p.o. | 2.0000 h | 2.6761 h | 407.0197 ng/mL | 2074.6687 ng·h/mL | 2078.5295 ng/mL·h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID (female, 6 weeks old, subcutaneous xenograft with 5×106 OCI-LY1 cells)[1]
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Dosage:50 mg/kg
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Administration:p.o.; daily; 17 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 37.2%.
Reduced BCL6 protein levels in harvested tumor tissues compared to vehicle-treated mice.
Caused no significant changes in body weight relative to the vehicle group throughout the treatment period.
Chemical Information
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Appearance Solid
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Molecular Weight 922.43
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Formula C46H52ClN11O8
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Color Light yellow to yellow
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SMILES
O=C1N(C(C2=CC(N3CCN(CC3)CC4CCN(CC4)C(C5CCN(C6=NC(NC7=CC(C=C8OCC(NC)=O)=C(C=C7)N(C)C8=O)=C(C=N6)Cl)CC5)=O)=CC=C21)=O)C9CCC(NC9=O)=O
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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
In Vitro:
DMSO : 100 mg/mL (108.41 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)
In Vivo:
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 (2.71 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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.
In Vivo Dissolution Calculator
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 (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0841 mL | 5.4205 mL | 10.8409 mL | 27.1023 mL |
| 5 mM | 0.2168 mL | 1.0841 mL | 2.1682 mL | 5.4205 mL | |
| 10 mM | 0.1084 mL | 0.5420 mL | 1.0841 mL | 2.7102 mL | |
| 15 mM | 0.0723 mL | 0.3614 mL | 0.7227 mL | 1.8068 mL | |
| 20 mM | 0.0542 mL | 0.2710 mL | 0.5420 mL | 1.3551 mL | |
| 25 mM | 0.0434 mL | 0.2168 mL | 0.4336 mL | 1.0841 mL | |
| 30 mM | 0.0361 mL | 0.1807 mL | 0.3614 mL | 0.9034 mL | |
| 40 mM | 0.0271 mL | 0.1355 mL | 0.2710 mL | 0.6776 mL | |
| 50 mM | 0.0217 mL | 0.1084 mL | 0.2168 mL | 0.5420 mL | |
| 60 mM | 0.0181 mL | 0.0903 mL | 0.1807 mL | 0.4517 mL | |
| 80 mM | 0.0136 mL | 0.0678 mL | 0.1355 mL | 0.3388 mL | |
| 100 mM | 0.0108 mL | 0.0542 mL | 0.1084 mL | 0.2710 mL |
PROTAC BCL6 Degrader-2 Related Classifications
HY-178803 Related Classifications
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