AT7519 trifluoroacetate

For research use only. Not for therapeutic Use.

  • CAT Number: I001661
  • CAS Number: 1431697-85-6
  • Molecular Formula: C18H18Cl2F3N5O4
  • Molecular Weight: 496.27
  • Purity: ≥95%
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AT7519 trifluoroacetate(Cat No.:I001661) is a potent and selective small molecule inhibitor of cyclin-dependent kinases (CDKs) with potential anticancer activity. By inhibiting CDKs, AT7519 trifluoroacetate disrupts the cell cycle progression and leads to cell cycle arrest and apoptosis in cancer cells. It targets multiple CDKs, including CDK1, CDK2, CDK4, and CDK9, which are involved in regulating cell division and transcriptional regulation. AT7519 trifluoroacetate has demonstrated promising activity against a variety of cancer types in preclinical studies and is being investigated in clinical trials for its potential as an anticancer therapy.


Catalog Number I001661
CAS Number 1431697-85-6
Synonyms

4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid

Molecular Formula C18H18Cl2F3N5O4
Purity ≥95%
Target Cyclin-Dependent Kinases
Solubility 10 mM in DMSO
Storage Store at -20°C
IC50 10-210 nM
IUPAC Name 4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide;2,2,2-trifluoroacetic acid
InChI InChI=1S/C16H17Cl2N5O2.C2HF3O2/c17-10-2-1-3-11(18)13(10)15(24)22-12-8-20-23-14(12)16(25)21-9-4-6-19-7-5-9;3-2(4,5)1(6)7/h1-3,8-9,19H,4-7H2,(H,20,23)(H,21,25)(H,22,24);(H,6,7)
InChIKey XTOQTRBZWZONHQ-UHFFFAOYSA-N
SMILES C1CNCCC1NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl.C(=O)(C(F)(F)F)O
Reference

<p style=/line-height:25px/>
<br>[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.
<br>[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.
<br>[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.
<br>[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.
<br>[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.
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