2. PROTAC Immunology/Inflammation
  3. PROTACs PD-1/PD-L1
  4. PROTAC PD-1/PD-L1 degrader-1

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.

For research use only. We do not sell to patients.

PROTAC PD-1/PD-L1 degrader-1 Chemical Structure

PROTAC PD-1/PD-L1 degrader-1 Chemical Structure

CAS No. : 2447066-37-5

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Based on 1 publication(s) in Google Scholar

PROTAC PD-1/PD-L1 degrader-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

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[1].

IC50 & Target[1]

Cereblon

 

In Vitro

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.

PROTAC PD-1/PD-L1 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1-10 μM
Incubation Time: 24 hours
Result: Reduced PD-L1 expression in a dose-dependent manner by 21% and 35% at 1 μM and 10 μM, respectively.
Molecular Weight

1076.59

Formula

C59H58ClN7O11
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9289 mL 4.6443 mL 9.2886 mL
5 mM 0.1858 mL 0.9289 mL 1.8577 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
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PROTAC PD-1/PD-L1 degrader-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC PD-1/PD-L1 degrader-12447066-37-5PROTACsPD-1/PD-L1PD-1/Programmed death-ligand 1degraderPROTACimmunitylysosome-dependentCD3TcellsMDA-MB-231Inhibitorinhibitorinhibit

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