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ABBV-744, a selective bromodomain and extra-terminal (BET) inhibitor

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ABBV-744, a selective bromodomain and extra-terminal (BET) inhibitor

 

 

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ABBV-744 is a selective bromodomain and extra-terminal (BET) inhibitor that preferentially bind to the 2nd

bromodomains (BD) than the 1st BD pf BET family proteins (i.e., BRD2. BRD3. BRD4) [1]. This selective

targeting of BD2 subsets of the BET bromodomain abolished the broad antiproliferative activities for previous

generation pan BET inhibitors, and only display antiproliferative activities in a limited number of cancer cell

lines, including acute myeloid leukaemia and prostate cancer that expressed the full-length androgen

receptor (AR) [2]. Improved tolerability is expected due to less impact on global transcription [3].

 

 

Details

Chemical Formula:

 

C28H30FN3O4

CAS No.:

 

2138861-99-9

Molecular Weight:

 

491.55

Purity:

 

> 98%

Appearance:

 

Grey

Chemical Name:

 

 

N-ethyl-4-(2-(4-fluoro-2,6-dimethylphenoxy)-5-(2-hydroxypropan-2-yl)phenyl)-6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridine-2-carboxamide

Solubility:

 

Up to 200 mM in DMSO

Synonyms:

 

ABBV 744, ABBV744

Storage:

 

For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.

 

References

 

1.

Sheppard G, et al. Discovery of ABBV-744, a first-in-class highly BDII-selective BET bromodomain inhibitor. Cancer Res 2018; 78(Suppl):Abstract nr 931. Pubmed ID: DOI: 10.1158/1538-7445.AM2018-931

2.

Faivre EJ, et al. Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer. Nature 2020; 578:306–310. Pubmed ID: 31969702

3.

Lin X, et al. ABBV-744, a first-in-class and highly selective inhibitor of the second bromodomain of BET family proteins, displays robust activities in preclinical models of acute myelogenous leukemia. Cancer Res 2018;78(13 Suppl):Abstract nr 800. Pubmed ID: DOI: 10.1158/1538-7445.AM2018-800

 

 

Ordering information

   

Catalog No.

Product Name

Size

C2874

ABBV-744

2mg, 10mg & 50mg

     

 

▣ 관련 페이지 ; Cellagen Technology

 

 

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