ABBV-744|CAS 2138861-99-9|BRD inhibitor

Cas No.:	2138861-99-9
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
Synonyms:	ABBV-744; ABBV 744; ABBV744；2138861-99-9
SMILES:	O=C(C(N1)=CC(C(C2=CC(C(C)(O)C)=CC=C2OC3=C(C)C=C(F)C=C3C)=CN4C)=C1C4=O)NCC
Formula:	C₂₈H₃₀FN₃O₄
M.Wt:	491.56
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS.
Target:	BET bromodomain[1]
In Vitro:	ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS[1].
References:	[1]. FIDANZE, Steven D., et al. BROMODOMAIN INHIBITORS. WO 2017177955 A1.

Cat. No.	Product name	Field of application
DC11452	ABBV-744	ABBV-744 is a BDII-selective BET bromodomain inhibitor that is being investigated to treat AML and metastic castration-resistant prostate cancer.BBV-744, a highly potent and selective inhibitor of the BD2 domain of BET family proteins with drug-like properties. In contrast to the broad range of cell growth inhibition induced by DbBi, the antiproliferative activity of ABBV-744 was largely, but not exclusively, restricted to cell lines of acute myeloid leukaemia and prostate cancer that expressed the full-length androgen receptor (AR). ABBV-744 retained robust activity in prostate cancer xenografts, and showed fewer platelet and gastrointestinal toxicities than the DbBi ABBV-07514.Analyses of RNA expression and chromatin immunoprecipitation followed by sequencing revealed that ABBV-744 displaced BRD4 from AR-containing super-enhancers and inhibited AR-dependent transcription, with less impact on global transcription compared with ABBV-075. These results underscore the potential value of selectively targeting the BD2 domain of BET family proteins for cancer therapy.