1610044-98-8
Chemical Structure
Amredobresib
Synonym(s): BI894999
- CAS No.: 1610044-98-8
- Formula:C26H29N9
- Molecular Weight:467.57
IUPAC Name: 6-(1-benzyl-6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)-N,3-dimethyl-[1,2,4]triazolo[4,3-a]pyrazin-8-amine
InChIKey: JLUUVUUYIXBDCG-UHFFFAOYSA-N
SMILES: CNC1=NC(C2=NC3=C(N2CC4=CC=CC=C4)C=C(N5CCN(CC5)C)C=C3)=CN6C(C)=NN=C16
Biological Activity: 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].
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Amredobresib | 98.97% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
