AT7519 trifluoroacetate Inhibitor CAS No. 1431697-85-6

Product Name	AT7519 trifluoroacetate
CAS No.	1431697-85-6
Molecular Weight	496.27
Formula	C₁₈H₁₈Cl₂F₃N₅O₄
Chemical Name	4-[(2,6-Dichlorobenzoyl)amino]-N-4-piperidinyl-1H-pyrazole-3-carboxamide 2,2,2-trifluoroacetate
Smiles	[nH]1nc(c(c1)NC(=O)c1c(cccc1Cl)Cl)C(=O)NC1CCNCC1 C(=O)(C(F)(F)F)O
Chemical Structure

Biological activities

AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7 ^[1]. In vitro, AT7519 is an ATP competitive CDK inhibitor with a Ki value of 38 nM for CDK1. AT7519 is inactive against all non-CDK kinases with the exception of GSK3? (IC50 = 89 nM). AT7519 shows potent antiproliferative activity in a variety of human tumor cell lines with IC50 values ranging from 40 nM for MCF-7 to 940 nM for SW620 consistent with the inhibition of CDK1 and CDK2 ^[2]. In vivo, it can be used by 10-20 mg/kg/day in mice ^[3].

References

[1]. Santo L, Vallet S, Hideshima T, 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, 29(16):2325-2336. [2]. Squires MS, Feltell RE, Wallis NG, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther. 2009, 8(2):324-332. [3]. Squires MS, Cooke L, Lock V, 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, 9(4):920-928.

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