1431697-85-6

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.

CDK9/Cyclin T: 10 nM (IC₅₀); CDK5/p35: 13 nM (IC₅₀); cdk2/cyclin A: 47 nM (IC₅₀); Cdk4/cyclin D1: 100 nM (IC₅₀); cdk6/cyclin D3: 170 nM (IC₅₀); Cdk1/cyclin B: 210 nM (IC₅₀); CDK7/Cyclin H/MAT1: 2400 nM (IC₅₀); GSK3β: 89 nM (IC₅₀)

Store at -20°C

[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. DOI:10.1038/onc.2009.510
[2] Squires MS, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. DOI:10.1158/1535-7163.MCT-08-0890
[3] 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. DOI:10.1158/1535-7163.MCT-09-1071