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; 578:306310. 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.
