产品
编 号:F186167
分子式:C25H33N5O3
分子量:451.56
产品类型
结构图
CAS No: 1564268-08-1
联系客服
产品详情
生物活性:
BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
体内研究:
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.Animal Model:Severe combined immunodeficiency (SCID) female mice (9-12 weeks old) inoculated subcutaneously into the right flank with 5×106 SU-DHL-8 cells/mouse suspended in 0.1 mL of matrigel or with O
Dosage:15 mg/kg (maximal tolerated dose).
Administration:Orally daily for 12 days (on day 21 post-tumour inoculation).
Result:Showed strong efficacy in the AML models THP-1, MOLM-13 and KG-1, with T/C between 13 and 20%. Also active in MM models in a human IGH-cyclin D1 translocated MOLP-8 model with a T/C of 3%.
体外研究:
BAY 1238097 shows strong inhibitory activity (IC50 BAY1238097 相关抗体: