2751721-40-9
中文名稱
化合物AZ5576
英文名稱
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
2024/11/01 22:00:17
2751721-40-9 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點(diǎn)617.5±55.0 °C(Predicted)
密度1.25±0.1 g/cm3(Predicted)
酸度系數(shù)(pKa)13.12±0.40(Predicted)
形態(tài)Solid
顏色White to off-white
應(yīng)用領(lǐng)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.