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[1][2][3][4][5].

Product Specifications

CAS Number

[1610044-98-8]

Product Name Alternative

BI894999

UNSPSC

12352005

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/amredobresib.html

Purity

98.97

Solubility

DMSO : 1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C26H29N9

Molecular Weight

467.57

References & Citations

[1]Ulrike Tontsch-Grunt, et al. Combination treatment of acute myeloid leukemia. Patent WO2019145410A1.|[2]Shaonan Wang, et al. Method for administration of an anti cancer agent. Patent WO2021175824A1.|[3]Tontsch-Grunt U, et al. Therapeutic impact of BET inhibitor BI 894999 treatment: backtranslation from the clinic. Br J Cancer. 2022 Aug;127 (3) :577-586.|[4]Tontsch-Grunt U, et al. Synergistic activity of BET inhibitor BI 894999 with PLK inhibitor volasertib in AML in vitro and in vivo. Cancer Lett. 2018 May 1;421:112-120.|[5]Gerlach D, et al. The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML. Oncogene. 2018 May;37 (20) :2687-2701.