PROTAC PD-1/PD-L1 degrader-1
Based on 1 Customer Validation
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
(Pink: PD-1/PD-L1 ligand (HY-131187); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.52%
- CAS No.: 2447066-37-5
- Formula: C59H58ClN7O11
- Molecular Weight:1076.59
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Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
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Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>10 μM
Compound: P22
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Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
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[PMID: 32388281] |
| B16-F10 | IC50 |
>10 μM
Compound: P22
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Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
Antiproliferative activity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
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[PMID: 32388281] |
| Jurkat | IC50 |
>10 μM
Compound: P22
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Antiproliferative activity against human jurkat cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human jurkat cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
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[PMID: 32388281] |
| MDA-MB-231 | IC50 |
>10 μM
Compound: P22
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Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
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[PMID: 32388281] |
| NCI-H1299 | IC50 |
>10 μM
Compound: P22
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Antiproliferative activity against human H1299 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human H1299 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
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[PMID: 32388281] |
PROTAC PD-1/PD-L1 degrader-1 (compound p22) reduces cell surface PD-L1 expression for more than 14%[1].
PROTAC PD-1/PD-L1 degrader-1 (1-10 μM; 24 hours) reduces PD-L1 expression in a dose-dependent manner by 21% and 35% at 1 μM and 10 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:1-10 μM
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Incubation Time:24 hours
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Result:Reduced PD-L1 expression in a dose-dependent manner by 21% and 35% at 1 μM and 10 μM, respectively.
Chemical Information
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CAS No. 2447066-37-5
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Appearance Solid
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Molecular Weight 1076.59
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Formula C59H58ClN7O11
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Color White to off-white
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SMILES
O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCC(N4CCN(C(C5N(CC6=CC(Cl)=C(OCC7=CC=CC(C8=CC=C9OCCOC9=C8)=C7C)C=C6OCC%10=CC=CC(C#N)=C%10)CCCC5)=O)CC4)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 210 mg/mL (195.06 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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: ≥ 1.4 mg/mL (1.30 mM); Clear solution
This protocol yields a clear solution of ≥ 1.4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.4 mg/mL (1.30 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.4 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (274 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 (sealed storage, away from moisture and light). 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 | 0.9289 mL | 4.6443 mL | 9.2886 mL | 23.2215 mL |
| 5 mM | 0.1858 mL | 0.9289 mL | 1.8577 mL | 4.6443 mL | |
| 10 mM | 0.0929 mL | 0.4644 mL | 0.9289 mL | 2.3221 mL | |
| 15 mM | 0.0619 mL | 0.3096 mL | 0.6192 mL | 1.5481 mL | |
| 20 mM | 0.0464 mL | 0.2322 mL | 0.4644 mL | 1.1611 mL | |
| 25 mM | 0.0372 mL | 0.1858 mL | 0.3715 mL | 0.9289 mL | |
| 30 mM | 0.0310 mL | 0.1548 mL | 0.3096 mL | 0.7740 mL | |
| 40 mM | 0.0232 mL | 0.1161 mL | 0.2322 mL | 0.5805 mL | |
| 50 mM | 0.0186 mL | 0.0929 mL | 0.1858 mL | 0.4644 mL | |
| 60 mM | 0.0155 mL | 0.0774 mL | 0.1548 mL | 0.3870 mL | |
| 80 mM | 0.0116 mL | 0.0581 mL | 0.1161 mL | 0.2903 mL | |
| 100 mM | 0.0093 mL | 0.0464 mL | 0.0929 mL | 0.2322 mL |
PROTAC PD-1/PD-L1 degrader-1 Related Classifications
HY-131183 Related Classifications
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