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ABBV-744

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Price:
$169.00
Catalog #:
C2874
Quantity:


Product Description

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].


Technical information:

Chemical Formula:   C28H30FN3O4
CAS #:   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

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.


Reference:

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

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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