产品
编 号：F161416
分子式：C18H18Cl2F3N5O4
分子量：496.27
分子式：C18H18Cl2F3N5O4
分子量：496.27
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 1431697-85-6
产品详情
生物活性：
AT7519 (AT7519M) TFA as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
体内研究：
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.
体外研究：
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. AT7519TFAalso inhibits transcription in human tumor cell lines. Furthermore, AT7519 TFA inhibits RNA polymerase II and reduces antiapoptotic protein levels.
AT7519 (AT7519M) TFA as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
体内研究：
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.
体外研究：
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. AT7519TFAalso inhibits transcription in human tumor cell lines. Furthermore, AT7519 TFA inhibits RNA polymerase II and reduces antiapoptotic protein levels.
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