2751721-40-9
中文名称
化合物AZ5576
英文名称
AZ5576
CAS
2751721-40-9
分子式
C21H24FN3O3
分子量
385.43
MOL 文件
2751721-40-9.mol
更新日期
2023/11/10 17:19:32
2751721-40-9 结构式
物理化学性质
沸点617.5±55.0 °C(Predicted)
密度1.25±0.1 g/cm3(Predicted)
酸度系数(pKa)13.12±0.40(Predicted)
形态Solid
颜色White to off-white
应用领域
用途一
AZ5576 is a potent and highly selective CDK9 inhibitor. Treatment with AZ5576 inhibited growth of DLBCL cell lines in vitro and in vivo, independent of cell-of-origin. CDK9 inhibition downregulated Mcl-1 and MYC mRNA transcript and protein in a dose-dependent manner. MYC-expressing cell lines demonstrated enhanced susceptibility to AZ5576. CDK9 inhibition promoted turnover of MYC protein, and decreased MYC phosphorylation at the stabilizing Ser62 residue and downregulated MYC transcriptional targets in DLBCL cells, a finding confirmed in a functional reporter assay, suggesting that CDK9 may govern MYC protein turnover, thus regulating its expression through multiple mechanisms.