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AT7519 Hydrochloride

CAS No. : 902135-91-5

MCE 国际站：AT7519 Hydrochloride

产品活性：AT7519 Hydrochloride 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 | Apoptosis

作用靶点：CDK | Apoptosis

In Vitro: AT7519 (0-4 µM) 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 overcomes proliferative advantage conferred by cytokines and the protective effect of BMSC. AT7519 (0.5 µM) induces apoptosis of MM cells in a time-dependent manner. Moreover, AT7519 (0.5 µM) inhibits phosphorylation of RNA polymerase II CTD and partially inhibits RNA synthesis in MM.1S cells. AT7519 (250 nM) inhibits cell cycle progression in human tumor cell lines. AT7519 also induces apoptosis of human tumor cell lines. AT7519 (100⁻⁷00 nM) induces apoptosis in leukemia cell lines. AT7519 also inhibits transcription in human tumor cell lines. Furthermore, AT7519 inhibits RNA polymerase II and reduces antiapoptotic protein levels.

In Vivo: AT7519 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.) also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice.

相关产品：Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | MG-132 | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Paclitaxel | Y-27632 dihydrochloride | Acetylcysteine | Angiotensin II human | SP600125 | 5-Fluorouracil | Staurosporine | Bortezomib | Tamoxifen | 2-Deoxy-D-glucose | Gemcitabine | Verteporfin | Decitabine | Actinomycin D | Temozolomide | BAY 11⁻⁷082 | Etoposide | Mitomycin C | CCCP | DAPT | Rotenone | Etomoxir | Stattic | Docetaxel | Fulvestrant

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