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BAY1238097

CAS No. : 1564268-08-1

MCE 站：BAY1238097

产品活性：BAY1238097 是一种有效的、BET 与组蛋白 结合的选择性抑制剂，通过下调c-Myc水平及下游转录组，在AML (急性髓性白血病) 和MM (多发性骨髓瘤) 模型中表现出较强的抗增殖活性 (IC₅₀ 值 <100 nM)。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: 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.
BAY 1238097 has in vitro anti-tumour activity in lymphoma models. BAY 1238097 affects the gene expression of GCB DLBCL cells. 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.

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

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