PROTAC PD-L1 degrader-1
Based on 1 publication(s) in Google Scholar
PROTAC PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC50 of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer.
(Pink: PD-1/PD-L1 ligand (HY-19745); Blue: Cereblon ligand (HY-150839); Black: linker).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.79%
- CAS 番号: 3052114-77-6
- 分子式: C45H55N5O7
- 分子量:777.95
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 PROTAC PD-L1 degrader-1
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生物活性
製品説明
(Pink: PD-1/PD-L1 ligand (HY-19745); Blue: Cereblon ligand (HY-150839); Black: linker).
IC50 & Target
[1]|
Cereblon 131.77 μM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
23.06 μM
Compound: PA8
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Antitumor activity against mouse 4T1 cells assessed as inhibition of cell viability incubated for 48 hrs by MTT assay
Antitumor activity against mouse 4T1 cells assessed as inhibition of cell viability incubated for 48 hrs by MTT assay
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[PMID: 38889052] |
体外実験
PROTAC PD-L1 degrader-1 (compound PA8; 0.078-10 μM; 24 h) displays a significant degradation effect on PD-L1 protein in
4T1 cells across in a dose-dependent manner[1].
PROTAC PD-L1 degrader-18 binds specifically to CRBN and PD-L1 with Kd values of 131.77 μM and 59.2 μM, respectively, and both are concentration dependent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:4T1 cells
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Concentration:0.078 μM, 0.156 μM, 0.312 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Displayed a significant degradation effect on PD-L1 protein in 4T1 cells.
体内実験
Pharmacokinetic Parameters of PROTAC PD-L1 degrader-1 (compound PA8) in Male Sprague-Dawley rats[1].
| Plasma PK properties | CL (mL/min/kg) | Vss (L/kg) (ng·h/mL) | Tmax (h) | Cmax (ng/mL) | T1/2 (h) |
| i.v (3 mg/kg) | 471.0 | 23.0 | / | / | 0.952 |
| i.p (30 mg/kg) | / | / | 2.0 | 217.0 | 5.3 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 week old female BALB/c mice injected with 4T1 cells[1].
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Dosage:30 and 60 mg/kg
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Administration:ip; once daily for 15 days
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Result:The antitumor effect can be obviously observed.
化学情報
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CAS 番号 3052114-77-6
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性状 Solid
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分子量 777.95
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分子式 C45H55N5O7
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Color White to off-white
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SMILES
O=C(NCCNCC1=CC=C(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)N=C1OC)CCCCCCCCNC(COC4=CC=C(C(CC5)C(NC5=O)=O)C=C4)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (128.54 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 (protect from 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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 (3.21 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.21 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 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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.
プロトコル
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
純度とドキュメンテーション
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データシート (269 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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取扱説明書 (2659 KB)
参考文献
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 (protect from 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 | 1.2854 mL | 6.4271 mL | 12.8543 mL | 32.1357 mL |
| 5 mM | 0.2571 mL | 1.2854 mL | 2.5709 mL | 6.4271 mL | |
| 10 mM | 0.1285 mL | 0.6427 mL | 1.2854 mL | 3.2136 mL | |
| 15 mM | 0.0857 mL | 0.4285 mL | 0.8570 mL | 2.1424 mL | |
| 20 mM | 0.0643 mL | 0.3214 mL | 0.6427 mL | 1.6068 mL | |
| 25 mM | 0.0514 mL | 0.2571 mL | 0.5142 mL | 1.2854 mL | |
| 30 mM | 0.0428 mL | 0.2142 mL | 0.4285 mL | 1.0712 mL | |
| 40 mM | 0.0321 mL | 0.1607 mL | 0.3214 mL | 0.8034 mL | |
| 50 mM | 0.0257 mL | 0.1285 mL | 0.2571 mL | 0.6427 mL | |
| 60 mM | 0.0214 mL | 0.1071 mL | 0.2142 mL | 0.5356 mL | |
| 80 mM | 0.0161 mL | 0.0803 mL | 0.1607 mL | 0.4017 mL | |
| 100 mM | 0.0129 mL | 0.0643 mL | 0.1285 mL | 0.3214 mL |
PROTAC PD-L1 degrader-1 関連分類
HY-163757 関連分類
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