PROTAC PD-L1 degrader-2
Based on 1 Customer Validation
PROTAC PD-L1 degrader-2 is a PD-L1 PROTAC degrader with an IC50 of 197.4 nM and a Kd of 301 nM. PROTAC PD-L1 degrader-2 induces PD-L1 endocytosis, drives degradation via the proteasomal and lysosomal pathways, and inhibits the PD-1/PD-L1 interaction. As an immune activator, PROTAC PD-L1 degrader-2 increases the levels of CD4+, CD8+, granzyme B and perforin. PROTAC PD-L1 degrader-2 can be used in studies related to colon cancer immunology.
(Pink: PD-1/PD-L1 ligand (HY-162973); Blue: Cereblon ligand (HY-W867704); Black: linker (HY-128833)).
For research use only. We do not sell to patients.
- Purity: 95.23%
- CAS No.: 2995357-09-8
- Formula: C46H42ClFN6O8
- Molecular Weight:861.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
PROTAC PD-L1 degrader-2 (Compound 9i) (1.25-20 μM; 24 h) induces concentration-dependent degradation of PD-L1 in HCC-827 cells, with a degradation rate of 60.87% after treatment at 20 μM for 24 h[1].
PROTAC PD-L1 degrader-2 (0.25-10 μM; 24 h) induces concentration-dependent degradation of PD-L1 in SK-N-AS, 786-O and MC38 cells, exhibiting broad-spectrum PD-L1 degradation activity[1].
PROTAC PD-L1 degrader-2 (1.25-10 μM; 24 h) enhances T cell-mediated killing of HCC-827 cells in a co-culture model, reduces the survival rate of HCC-827 cells to 50.65% after treatment at 10 μM for 24 h, and exhibits low cytotoxicity against Jurkat cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human non-small cell lung cancer HCC-827 cells
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Concentration:1.25, 2.5, 5, 10 and 20 μM
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Incubation Time:24 h
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Result:Induced concentration-dependent degradation of PD-L1 in HCC-827 cells.
Achieved a 60.87% degradation rate at 20 μM after 24 h.
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Cell Line:human neuroblastoma SK-N-AS cells, human renal carcinoma 786-O cells, mouse colon cancer MC38 cells
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Concentration:0.25, 1.25, 2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:Induced concentration-dependent degradation of PD-L1 in all three cell lines.
Reduced PD-L1 levels significantly in SK-N-AS cells at concentrations ≥ 1.25 μM.
Reduced PD-L1 levels significantly in 786-O cells at concentrations ≥ 2.5 μM.
Reduced PD-L1 levels significantly in MC38 cells at 10 μM.
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Cell Line:HCC-827/Jurkat cell co-culture model
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Concentration:1.25, 2.5, 5, 10 and 20 μM
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Incubation Time:24 h
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Result:Reduced HCC-827 cell survival rate to 50.65% at 10 μM in the co-culture system, indicating enhanced Jurkat-mediated tumor cell killing.
Showed negligible toxicity to Jurkat cells at concentrations ≤ 10 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 6 weeks old, 18-22 g, subcutaneous inoculation of MC38 colon cancer cells)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; daily; 15 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 48.72% at 10 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 57.35% at 20 mg/kg.
Significantly downregulated PD-L1 protein levels in tumor tissues.
Increased mRNA expression of immune chemokines CXCR3, CXCL9, and CXCL10.
Elevated the CD8+/CD4+ T cell ratio in lymph nodes and tumor tissue.
Increased granzyme B and perforin expression in tumor tissues.
Caused no significant changes in body weight, organ histology (H&E staining), or blood parameters, indicating no obvious toxicity.
Chemical Information
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CAS No. 2995357-09-8
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Appearance Solid
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Molecular Weight 861.31
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Formula C46H42ClFN6O8
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Color Light yellow to yellow
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SMILES
ClC1=C(C=CC=C1C2=CC=CC=C2F)COC3=CC(OCC4=CC(C#N)=CN=C4)=C(C=C3)CNCCOCCOCCNC5=C(C6=CC=C5)C(N(C6=O)C7C(NC(CC7)=O)=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
DMSO : 100 mg/mL (116.10 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)
Purity & Documentation
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Data Sheet (275 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 |
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| DMSO | 1 mM | 1.1610 mL | 5.8051 mL | 11.6102 mL | 29.0256 mL |
| 5 mM | 0.2322 mL | 1.1610 mL | 2.3220 mL | 5.8051 mL | |
| 10 mM | 0.1161 mL | 0.5805 mL | 1.1610 mL | 2.9026 mL | |
| 15 mM | 0.0774 mL | 0.3870 mL | 0.7740 mL | 1.9350 mL | |
| 20 mM | 0.0581 mL | 0.2903 mL | 0.5805 mL | 1.4513 mL | |
| 25 mM | 0.0464 mL | 0.2322 mL | 0.4644 mL | 1.1610 mL | |
| 30 mM | 0.0387 mL | 0.1935 mL | 0.3870 mL | 0.9675 mL | |
| 40 mM | 0.0290 mL | 0.1451 mL | 0.2903 mL | 0.7256 mL | |
| 50 mM | 0.0232 mL | 0.1161 mL | 0.2322 mL | 0.5805 mL | |
| 60 mM | 0.0194 mL | 0.0968 mL | 0.1935 mL | 0.4838 mL | |
| 80 mM | 0.0145 mL | 0.0726 mL | 0.1451 mL | 0.3628 mL | |
| 100 mM | 0.0116 mL | 0.0581 mL | 0.1161 mL | 0.2903 mL |
PROTAC PD-L1 degrader-2 Related Classifications
HY-162972 Related Classifications
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