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PROTAC BCL6/GSPT1 Degrader-1

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PROTAC BCL6/GSPT1 Degrader-1 is a dual-target PROTAC degrader aimed at BCL6 and GSPT1. It inhibits cell proliferation, promotes DNA damage, and induces cell cycle arrest and apoptosis (apoptosis) in diffuse large B cell lymphoma. PROTAC BCL6/GSPT1 Degrader-1 is applicable for research in tumors such as lymphoma.

PROTAC BCL6/GSPT1 Degrader-1

Cas No. 3039500-55-2
Pack SizePriceUSA StockGlobal StockQuantity
10 mgInquiryInquiryInquiry
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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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Product Introduction

Bioactivity
Description
PROTAC BCL6/GSPT1 Degrader-1 is a dual-target PROTAC degrader aimed at BCL6 and GSPT1. It inhibits cell proliferation, promotes DNA damage, and induces cell cycle arrest and apoptosis (apoptosis) in diffuse large B cell lymphoma. PROTAC BCL6/GSPT1 Degrader-1 is applicable for research in tumors such as lymphoma.
In vitro
PROTAC BCL6/GSPT1 Degrader-1 (Compound A5) effectively degrades BCL6 (DC50: 0.48 nM) and GSPT1 in Farage DLBCL cells in a time- and concentration-dependent manner at concentrations ranging from 0-10000 nM over 0-72 hours. At 0.1-10 μM for 72 hours, it inhibits the proliferation of Farage diffuse large B-cell lymphoma (DLBCL) cells (IC50: 0.413) and induces DNA damage. Additionally, at concentrations of 0.1-2.5 μM over 72 hours, it promotes apoptosis and cell cycle arrest in these cells.
In vivo
PROTAC BCL6/GSPT1 Degrader-1 (10 mg/kg; i.p.; daily; 3 days) effectively degrades BCL6 and GSPT1 in Farage xenograft tumors in NOD/SCID mice.
Chemical Properties
Molecular Weight1005.47
FormulaC47H57ClN10O13
Cas No.3039500-55-2
SmilesO=C(NC)COC1=CC=2C=C(C=C(OC)C2N(C1=O)C)NC3=NC(=NC=C3Cl)N4CCC(C(=O)NCCOCCOCCOCCOCCNC5=CC=CC=6C(=O)N(C(=O)C56)C7C(=O)NC(=O)CC7)CC4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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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:
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2 Enter the in vivo formulation:
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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
Related Tags: PROTAC BCL6/GSPT1 Degrader-1 in vivo | PROTAC BCL6/GSPT1 Degrader-1 in vitro | PROTAC BCL6/GSPT1 Degrader-1 formula | PROTAC BCL6/GSPT1 Degrader-1 molecular weight