AT7519

• CAT Number: I005048
• CAS Number: 844442-38-2
• Molecular Formula: C16H17Cl2N5O2
• Molecular Weight: 382.24
• Purity: ≥95%
• Target: Cyclin-Dependent Kinases
• Solubility: DMSO ≥22mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
• Storage: 3 years -20C powder
• IC50: 10-210 nM

AT7519 (CAT: I005048) is a small molecule inhibitor that targets multiple cyclin-dependent kinases (CDKs). CDKs are enzymes that play a crucial role in cell cycle regulation and are involved in various cellular processes, including cell division, proliferation, and transcriptional regulation. AT7519 inhibits CDK1, CDK2, CDK4, and CDK9, among others, which leads to cell cycle arrest and inhibition of tumor cell growth. It has shown potential as an anticancer agent in preclinical studies, demonstrating efficacy against a wide range of cancer types, including solid tumors and hematological malignancies. AT7519 has also been studied in combination with other anticancer agents and as a sensitizer to radiation therapy.

Reference

[1]. Santo L, Vallet S, Hideshima T, Cirstea D, Ikeda H, Pozzi S, Patel K, Okawa Y, Gorgun G, Perrone G, Calabrese E, Yule M, Squires M, Ladetto M, Boccadoro M, Richardson PG, Munshi NC, Anderson KC, Raje N.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. Epub 2010 Jan 25.

[2]. Squires MS, Feltell RE, Wallis NG, Lewis EJ, Smith DM, Cross DM, Lyons JF, Thompson NT.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. Epub 2009 Jan 27.

[3]. Squires MS, Cooke L, Lock V, Qi W, Lewis EJ, Thompson NT, Lyons JF, Mahadevan D.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. Epub 2010 Mar 30.

[4]. Mahadevan D, Plummer R, Squires MS, Rensvold D, Kurtin S, Pretzinger C, Dragovich T, Adams J, Lock V, Smith DM, Von Hoff D, Calvert H.A phase I pharmacokinetic and pharmacodynamic study of AT7519, a cyclin-dependent kinase inhibitor in patients with refractory solid tumors.Ann Oncol. 2011 Sep;22(9):2137-43. Epub 2011 Feb 16.

[5]. Wyatt PG, Woodhead AJ, Berdini V, Boulstridge JA, Carr MG, Cross DM, Davis DJ, Devine LA, Early TR, Feltell RE, Lewis EJ, McMenamin RL, Navarro EF, O/’Brien MA, O/’Reilly M, Reule M, Saxty G, Seavers LC, Smith DM, Squires MS, Trewartha G, Walker MT, Woolford AJ.Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.J Med Chem. 2008 Aug 28;51(16):4986-99. Epub 2008 Jul 26.