BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different MM (multiple myeloma) and AML (acute myeloid leukemia) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50<100 nM).

BAY 1238097 has in vitro anti-tumour activity in lymphoma models. BAY 1238097 affects the gene expression of GCB DLBCL cells. BAY 1238097 shows strong inhibitory activity (IC50< 100 nM) in a TR-FRET assay using BET BRD4 bromodomain 1 and an acetylated peptide derived from histone H4. In the NanoBRET assay, the interaction between BRD4 (IC50=63 nM), BRD3 or BRD2 (IC50=609 nM) and H4 (IC50=2430 nM) is inhibited[1]. At the gene level, BTK, CCDC86, CCND2, CD19, CD27, FAIM, FCMR (FAIM3), IL7R, IRAK1, MAPK13, MYB, MYC, PDE4B, TNFRSF13B, TNFRSF17 are among the top downregulated genes. Beside histone-coding genes, the upregulated genes include CCL5, CDKN2C, CD69, JUN, and MKNK2[2].

BAY 1238097 is well tolerated at 10-15 mg/kg applied daily over 9-14 days in different disease models, with no obvious toxicity[1][2] and it shows strong efficacy in the AML and MM models. BAY 1238097 has in vivo anti-tumour activity in lymphoma models[1][2].

1564268-08-1

C25H33N5O3

451.56

BAY1238097

DMSO:150 mg/mL (332.18 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years