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Amredobresib

Name: Amredobresib
Brand: TargetMol
SKU: T39073
Rating: 4.5 (1 reviews)

(Synonyms: BI-894999, BI894999, BI 894999) Copy Product Info

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Synonyms: BI-894999, BI894999, BI 894999

Catalog No. T39073 Copy Product Info

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Amredobresib is an orally active BET inhibitor that binds to the acetyl-lysine recognition domains of proteins such as BRD2/3/4, exhibiting anti-tumor activity. Amredobresib is currently in clinical research stages for evaluating its therapeutic potential in various solid tumors and hematological malignancies.

Cas No. 1610044-98-8

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Product Introduction

Bioactivity

Description	Amredobresib is an orally active BET inhibitor that binds to the acetyl-lysine recognition domains of proteins such as BRD2/3/4, exhibiting anti-tumor activity. Amredobresib is currently in clinical research stages for evaluating its therapeutic potential in various solid tumors and hematological malignancies.
Targets & IC50	BRD4 BD2:41 nM
In vitro	Amredobresib inhibits the proliferation of nuclear transcription regulatory domain (NUT) cancer (NC) cell lines [3]. Amredobresib (10–30 nM; 30 min) causes rapid dissociation of BRD4-NUT from chromatin in the NC cell line Ty-82 [3]. Amredobresib (3.3–30 nM; 24–72 h) induces G1 phase arrest in MV-4-11B cells [4]. Amredobresib inhibits the binding of the bromo domains of BRD4-BD1 and BRD4-BD2 to acetylated histones, with IC₅₀ values of 5 nM and 41 nM, respectively [5].
In vivo	Amredobresib (2 mg/kg; oral; daily) inhibits tumor growth in a mouse xenograft model of NUT cancer (NC)[3]. Amredobresib (2–4 mg/kg; oral; daily) inhibits tumor growth and prolongs survival in a mouse model of human MV-4-11B AML cells transplanted via intravenous injection[4].
Synonyms	BI-894999, BI894999, BI 894999

Chemical Properties

Molecular Weight	467.58
Formula	C₂₆H₂₉N₉
Cas No.	1610044-98-8
Smiles	N=1N=C(N2C=C(N=C(NC)C12)C3=NC=4C=CC(=CC4N3CC=5C=CC=CC5)N6CCN(C)CC6)C

Storage & Solubility Information

Storage	Keep away from moistureKeep 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: < 1 mg/mL (insoluble)

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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:

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.

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Keywords

Amredobresib

Related Tags: Amredobresib chemical structure | Amredobresib in vivo | Amredobresib in vitro | Amredobresib formula | Amredobresib molecular weight