BAY1238097, a potent and selective bromodomain and extra-terminal motif (BET) inhibitor with anticancer activity, exhibits strong antiproliferative effects in AML (Acute Myeloid Leukemia) and MM (Multiple Myeloma) models. BAY1238097 is useful for studying advanced refractory malignancies.

BRD3(BRD2):609 nM, H4:2430 nM, BRD4:63 nM, BET:< 100 nM (TR-FRET assay)

BAY 1238097 exhibits potent inhibitory activity (IC50 < 100 nM) in a TR-FRET assay utilizing BET BRD4 bromodomain 1 and an acetylated peptide derived from histone H4. In the NanoBRET assay, it inhibits the interaction between BRD4 (IC50=63 nM), BRD3, or BRD2 (IC50=609 nM), and H4 (IC50=2430 nM)[2].
BAY 1238097 demonstrates in vitro anti-tumor activity in lymphoma models. It influences the gene expression of GCB DLBCL cells. At the gene level, top downregulated genes include BTK, CCDC86, CCND2, CD19, CD27, FAIM, FCMR (FAIM3), IL7R, IRAK1, MAPK13, MYB, MYC, PDE4B, TNFRSF13B, TNFRSF17. In addition to histone-coding genes, upregulated genes include CCL5, CDKN2C, CD69, JUN, and MKNK2[1].

BAY 1238097 demonstrates robust efficacy in AML and MM models. It exhibits in vivo anti-tumor activity in lymphoma models[1][2].
BAY 1238097 is well tolerated at doses of 10-15 mg/kg administered daily over 9-14 days in various disease models, with no apparent toxicity[1][2].