AT7519(AT 7519) CDK抑制剂|CAS 844442-38-2（53273ES）

AT7519 (AT 7519)是一种有效的CDK小分子抑制剂，作用于CDK1/2/4/5/6/9的IC₅₀值分别为210、47、100、13、170和<10 nM，通过调节细胞周期抑制多种癌症细胞增殖，表现出潜在的抗肿瘤活性。AT7519对CDK3和7及其他非CDK激酶无抑制活性。AT7519以ATP竞争性方式抑制CDK1，K_i值为38 nM。此外，AT7519也可抑制GSK3β，IC₅₀值为89 nM。

参考文献

1. Santo L, et al. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition. Oncogene. 2010 Apr 22;29(16):2325-36.
2. Squires MS, et al. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples. Mol Cancer Ther. 2010 Apr;9(4):920-8.
3. Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther. 2009 Feb;8(2):324-32.

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