Medchemexpress LLC 6-(2-(2,4-Difluorophenoxy)-5-((ethylsulfonyl)methyl)pyridin-3-yl)-8-methylpyrrolo[1,2-a]pyrazin-1(2H)-one | 2411226-02-1 | 99.7% | 10 MM * 1 ML

Supplier:  Medchemexpress LLC HY13106110MM/1ML

BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. It binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). This inhibitor also demonstrates anti-cancer activity.

• Orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor.
• Binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities.
• Exhibits anti-cancer activity.
• Demonstrates antiproliferative activity against various human leukemia and myeloma cell lines.
• Induces G1-phase cell cycle arrest and reduces c-Myc, BCL-2, and CDK6 expressions in MV-4-11 cells.
• Offers high selectivity for the BET bromodomain family.
• Shows strong antitumor activities in an MV4-11 mouse xenograft model.

Catalog No. 50-003-40701