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Homo-PROTAC cereblon degrader 1

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Catalog No. T13721Cas No. 2244520-98-5

Homo-PROTAC cereblon degrader 1 is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.

Homo-PROTAC cereblon degrader 1

Homo-PROTAC cereblon degrader 1

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Purity: 98.3%
Catalog No. T13721Cas No. 2244520-98-5
Homo-PROTAC cereblon degrader 1 is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$71In StockIn Stock
2 mg$98In StockIn Stock
5 mg$172In StockIn Stock
10 mg$297In StockIn Stock
25 mg$455In StockIn Stock
50 mg$728In StockIn Stock
100 mg$1,160In StockIn Stock
200 mg$1,560InquiryInquiry
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Batch Information

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Purity:98.3%
Appearance:Solid
Color:Yellow
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COA HNMR HPLC

Product Introduction

Homo-PROTAC cereblon degrader 1 AI Summary
Homo-PROTAC cereblon degrader 1 exhibits Protac activity at CRBN/IKZF1 in human MM1S cells and VHL/CRBN in HEK293 and human HeLa cells. In MM1S cells, its activity was assessed as IKZF1 degradation by measuring the IKZF1/tubulin ratio at 0.1 µM after 16 hours via Western blot analysis, resulting in a ratio of 79.0 relative to tubulin. In HEK293 and HeLa cells, it significantly alters the abundance of various proteins, including pVHL19, pVHL30, and CRBN, with activity ranging from 25.0% to 109.0% at different concentrations and time points. This indicates the compound's potential bioactivity in modulating protein levels related to both the CRBN/IKZF1 and VHL/CRBN pathways..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Homo-PROTAC cereblon degrader 1 is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.
In vitro
Homo-PROTAC cereblon degrader 1 (0-1 μM, 16 hours) effectively reduces Cereblon protein levels in the multiple myeloma cell line NCI-H929. Experimental results indicate that the effect is observed at a concentration of 10 nM after 16-hour incubation. The degradation efficiency reaches its peak at concentrations between 100 nM and 1 μM. However, when the concentration is further increased to 100 μM, the degradation of Cereblon is completely inhibited [1].
When MM1S cells were treated with Homo-PROTAC cereblon degrader 1 (100 nM, 0-24 hours), cereblon protein levels decreased within 15 minutes and peaked at 6 hours [1].
The effects of homo-PROTAC cerebrone degrader 1 (0-10 μM, 4 days) on the proliferation of palomidomide-sensitive multiple myeloma cell lines MM1S, NCI-H929, LP-1, KMS27, and RPMI 8226 were investigated. The results showed that Homo-PROTAC cereblon degrader 1 had little effect on the proliferation of the cells at concentrations of ≤1 μM [1].
Chemical Properties
Molecular Weight660.63
FormulaC32H32N6O10
Cas No.2244520-98-5
SmilesO=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2NCCOCCOCCNC4=C5C(C(=O)N(C5=O)C6C(=O)NC(=O)CC6)=CC=C4
Relative Density.1.527 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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 (302.74 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (7.57 mM), Sonication is recommended.
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
1mg5mg10mg50mg
1 mM1.5137 mL7.5685 mL15.1371 mL75.6853 mL
5 mM0.3027 mL1.5137 mL3.0274 mL15.1371 mL
10 mM0.1514 mL0.7569 mL1.5137 mL7.5685 mL
20 mM0.0757 mL0.3784 mL0.7569 mL3.7843 mL
50 mM0.0303 mL0.1514 mL0.3027 mL1.5137 mL
100 mM0.0151 mL0.0757 mL0.1514 mL0.7569 mL

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

PROTACsInhibitorinhibitHomo-PROTAC cereblon degrader 1HomoPROTAC cereblon degrader 1Homo PROTAC cereblon degrader 1Cereblon
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