2. Epigenetics
  3. Epigenetic Reader Domain
  4. Amredobresib

Amredobresib (BI894999) is an orally active BET inhibitor. Amredobresib inhibits the binding of BRD4-BD1 and BRD4-BD2 bromodomains to acetylated histones with IC50 values of 5 nM and 41 nM, respectively. Amredobresib exhibits anticancer activity against acute myeloid leukemia (AML) and NUT cancer.

For research use only. We do not sell to patients.

The Amredobresib was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

Amredobresib Chemical Structure

Amredobresib Chemical Structure

CAS No. : 1610044-98-8

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Based on 1 publication(s) in Google Scholar

Amredobresib Related Antibodies

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Description

Amredobresib (BI894999) is an orally active BET inhibitor. Amredobresib inhibits the binding of BRD4-BD1 and BRD4-BD2 bromodomains to acetylated histones with IC50 values of 5 nM and 41 nM, respectively. Amredobresib exhibits anticancer activity against acute myeloid leukemia (AML) and NUT cancer[1][2][3][4][5].

IC50 & Target

BET[1]
In Vitro

Amredobresib inhibits the proliferation of NUT carcinoma (NC) cell lines[3].
Amredobresib (10-30 nM; 30 min) causes the rapid detachment of BRD4-NUT from chromatin in NC cell line Ty-82[3].
Amredobresib (3.3-30 nM; 24-72 h) causes G1 arrest in MV-4-11B cells[4].
Amredobresib inhibits the binding of the BRD4-BD1 and BRD4-BD2 bromodomains to acetylated histones with IC50 values of 5 nM and 41 nM, respectively[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Amredobresib Related Antibodies
In Vivo

Amredobresib (2 mg/kg; p.o.; once daily) inhibits tumor growth in mouse models of NUT carcinoma (NC) xenografts[3].
Amredobresib (2-4 mg/kg; p.o.; daily) inhibits tumor growth and prolongs survival in mouse models engrafted intravenously with human MV-4-11B AML cells[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 week old, female CIEA-NOG mice (NOD.Cg-PrkdcscidIL2rgtm1Sug/JicTac) engrafted intravenously with human luciferase labeled MV-4-11B cells[4]
Dosage: 2 mg/kg or 4 mg/kg
Administration: Oral gavage (p.o.); daily
Result: Resulted in tumor growth inhibition (TGI) of 96% and survival prolongation of 29.5 days at 2 mg/kg.
Resulted in a TGI of 99% and survival prolongation of 52 days at 4 mg/kg.
Molecular Weight

467.57

Formula

C26H29N9
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CNC1=NC(C2=NC3=C(N2CC4=CC=CC=C4)C=C(N5CCN(CC5)C)C=C3)=CN6C(C)=NN=C16
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 0.5 mg/mL (1.07 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMSO : 0.5 mg/mL (1.07 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1387 mL 10.6936 mL 21.3872 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / DMSO 1 mM 2.1387 mL 10.6936 mL 21.3872 mL 53.4679 mL
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Amredobresib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Amredobresib1610044-98-8BI894999BI 894999BI-894999Epigenetic Reader DomainBETbromodomainacetylated lysinehistone H3histone H4gene transcriptionacute myeloid leukemiaAMLcancerInhibitorinhibitorinhibit

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