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AR/BRD4 RIPTAC-1

(Synonyms: Antiproliferative agent-71) Copy Product Info
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Synonyms: Antiproliferative agent-71

Catalog No. T211016 Copy Product Info
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AR/BRD4 RIPTAC-1 (Compound II-5) is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 holds promise for use in prostate cancer research. AR/BRD4 RIPTAC-1 is additionally applicable in molecular oncology research for investigating androgen receptor–epigenetic regulator interactions and for studying proximity-induced protein complex formation mechanisms in tumor-associated transcriptional regulation systems.
AR/BRD4 RIPTAC-1
Cas No. 3083307-42-7
Pack SizePriceUSA StockGlobal StockQuantity
1 mg$5647-10 days7-10 days
5 mg$1,1307-10 days7-10 days
10 mg$1,5807-10 days7-10 days
1 mL x 10 mM (in DMSO)$2,2507-10 days7-10 days
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.
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Product Introduction

Bioactivity
Description
AR/BRD4 RIPTAC-1 (Compound II-5) is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 holds promise for use in prostate cancer research. AR/BRD4 RIPTAC-1 is additionally applicable in molecular oncology research for investigating androgen receptor–epigenetic regulator interactions and for studying proximity-induced protein complex formation mechanisms in tumor-associated transcriptional regulation systems.
Targets & IC50
T47D cells:<0.5 μM (GI50)
In vitro
Methods:T47D cells were cultured in vitro and treated with AR/BRD4 RIPTAC-1 (Antiproliferative agent-71) for 72 hours, then the half-maximal growth inhibitory concentration GI₅₀ was determined.
Results:AR/BRD4 RIPTAC-1 (Antiproliferative agent-71) inhibited the growth of T47D cells with a GI₅₀ lower than 0.5 μM [1].
In vivo
Methods:CB17.SCID mice bearing VCaP tumors were orally administrated for 7 consecutive days, and tumor growth was monitored.
Results:AR/BRD4 RIPTAC-1 (Antiproliferative agent-71) effectively inhibited tumor proliferation in vivo [1].
SynonymsAntiproliferative agent-71
Chemical Properties
Molecular Weight907.09
FormulaC50H54N10O5S
Cas No.3083307-42-7
SmilesO(C1CC2(C1)CCN(CC2)C=3N=CC(C(N[C@H]4C(C)(C)[C@H](OC5=CC(OC)=C(C#N)C=C5)C4(C)C)=O)=CN3)C6=CC=C(C=C6)C=7C8=C(N9C([C@H](CC%10=NC=CO%10)N7)=NN=C9C)SC(C)=C8C
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: 40 mg/mL (44.1 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.1024 mL5.5121 mL11.0243 mL55.1213 mL
5 mM0.2205 mL1.1024 mL2.2049 mL11.0243 mL
10 mM0.1102 mL0.5512 mL1.1024 mL5.5121 mL
20 mM0.0551 mL0.2756 mL0.5512 mL2.7561 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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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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µL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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: AR/BRD4 RIPTAC-1 chemical structure | AR/BRD4 RIPTAC-1 in vivo | AR/BRD4 RIPTAC-1 in vitro | AR/BRD4 RIPTAC-1 formula | AR/BRD4 RIPTAC-1 molecular weight