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PROTAC PD-1/PD-L1 degrader-1

Name: PROTAC PD-1/PD-L1 degrader-1
Brand: TargetMol
SKU: T40112
Price: 253 USD
Availability: InStock
Rating: 5 (10 reviews)

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Synonyms:

Catalog No. T40112 Copy Product Info

Purity: 99.07%

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PROTAC PD-1/PD-L1 degrader-1, a Cereblon E3 ligand-based compound, is a PD-1/PD-L1 PROTAC that effectively inhibits the PD-1/PD-L1 interaction with an IC50 of 39.2 nM. It restores the suppressed immune response in a co-culture model of Hep3B/OS-8/hPD-L1 cells and CD3 T cells and moderately decreases PD-L1 protein levels through a lysosome-dependent mechanism.

Cas No. 2447066-37-5

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Pack Size	Price	USA Stock	Global Stock
1 mg	$253	In Stock	In Stock
5 mg	$619	In Stock	In Stock
10 mg	$987	-	In Stock
25 mg	$1,520	-	In Stock
50 mg	$1,980	-	In Stock
100 mg	$2,770	-	In Stock
200 mg	$3,730	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Batch Information

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Purity:99.07%

Appearance:Solid

Color:Yellow

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	PROTAC PD-1/PD-L1 degrader-1, a Cereblon E3 ligand-based compound, is a PD-1/PD-L1 PROTAC that effectively inhibits the PD-1/PD-L1 interaction with an IC50 of 39.2 nM. It restores the suppressed immune response in a co-culture model of Hep3B/OS-8/hPD-L1 cells and CD3 T cells and moderately decreases PD-L1 protein levels through a lysosome-dependent mechanism.
In vitro	PROTAC PD-1/PD-L1 degrader-1 (compound p22) significantly reduces PD-L1 expression on the cell surface by over 14%[1]. When administered at 1-10 μM for 24 hours, it decreases PD-L1 levels dose-dependently, with reductions of 21% and 35% at 1 μM and 10 μM, respectively[1]. Western Blot Analysis in MDA-MB-231 cell lines confirmed its efficacy in modulating PD-L1 expression at these dosages[1].

Chemical Properties

Molecular Weight	1076.59
Formula	C₅₉H₅₈ClN₇O₁₁
Cas No.	2447066-37-5
Smiles	N#CC1=CC=CC(=C1)COC2=CC(OCC3=CC=CC(C4=CC=C5OCCOC5=C4)=C3C)=C(Cl)C=C2CN6CCCCC6C(=O)N7CCN(C(=O)CCCC(=O)NC8=CC=CC=9C(=O)N(C(=O)C89)C%10C(=O)NC(=O)CC%10)CC7
Relative Density.	1.45 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 200 mg/mL (185.77 mM)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (9.29 mM), Suspension.

10% DMSO+90% Saline: < 10 mg/mL (9.29 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	0.9289 mL	4.6443 mL	9.2886 mL	46.4429 mL
5 mM	0.1858 mL	0.9289 mL	1.8577 mL	9.2886 mL
10 mM	0.0929 mL	0.4644 mL	0.9289 mL	4.6443 mL
20 mM	0.0464 mL	0.2322 mL	0.4644 mL	2.3221 mL
50 mM	0.0186 mL	0.0929 mL	0.1858 mL	0.9289 mL
100 mM	0.0093 mL	0.0464 mL	0.0929 mL	0.4644 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

PROTAC PD-1/PD-L1 degrader-1PROTAC PD-1/PD-L-1 degrader-1PROTAC PD1/PDL1 degrader1PROTAC PD 1/PD L1 degrader 1PROTACPD-L1PDL1PD-1/PD-L1PD1/PDL1PD-1PD1

Related Tags: PROTAC PD-1/PD-L1 degrader-1 chemical structure | PROTAC PD-1/PD-L1 degrader-1 in vitro | PROTAC PD-1/PD-L1 degrader-1 formula | PROTAC PD-1/PD-L1 degrader-1 molecular weight