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AT7519 TFA

CAS No. : 1431697-85-6

MCE 国际站：AT7519 TFA

产品活性：AT7519 (AT7519M) TFA 是一种有效的 CDK 抑制剂，对 CDK1，CDK2，CDK4-CDK6 以及 CDK9 的 IC₅₀ 值分别为 210，47，100，13，170 和 <10 nM。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

In Vitro: AT7519 (0-4 μM) TFA results in dose-dependent cytotoxicity with IC₅₀s ranging from 0.5 to 2 μM in MM cells, and this induced cytotoxicity is associated with GSK-3β activation independent of transcriptional inhibition. AT7519 TFA overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 μM) TFA induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 μM) TFA inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells. AT7519 (250 nM) TFA inhibits cell cycle progression in human tumor cell lines. AT7519 TFA also induces apoptosis of human tumor cell lines. AT7519 (100-700 nM) TFA induces apoptosis in leukemia cell lines. AT7519TFA also inhibits transcription in human tumor cell lines. Furthermore, AT7519 TFA inhibits RNA polymerase II and reduces antiapoptotic protein levels.

In Vivo: AT7519 TFA inhibits tumor growth in a human MM xenograft mouse model. AT7519 (4.6 and 9.1 mg/kg/dose) inhibits the growth of early-stage HCT116 tumor xenografts. AT7519 (10 mg/kg, i.p.) TFA also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice.

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