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AT7519

multi-CDK inhibitor

AT7519

Catalog No. A5719
Size Price Stock Qty
5mg $80.00 In stock
25mg $250.00 In stock
100mg $680.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

AT7519

Biological Activity

Description AT7519 is a inhibitor of CDK1, 2, 4, 5, 6 and 9 with IC50 values of 10-210 nM.
Targets CDK9/CyclinT CDK5/p35 CDK2/CyclinA GSK-3β CDK4/CyclinD1 CDK6/CyclinD3
IC50 <10 nM 13 nM 47 nM 89 nM 100 nM 170 nM

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Chemical Properties

Cas No. 844442-38-2 SDF Download SDF
Chemical Name 4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide
Canonical SMILES C1CNCCC1NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl
Formula C16H17Cl2N5O2 M.Wt 382.24
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

AT7519 is a small-molecule inhibitor of cyclin-dependent kinases (CDKs) with IC50 values of 210, 47, 100, 13, 170 and <10 nM for CDK1, CDK2, CDK4, CDK5, CDK6 and CDK9, respectively [1].

AT7519 showed no inhibition activity against CDK3, 7 and other non-CDK kinases. It inhibited CDK1 in an ATP- competitive manner with Ki value of 38 nM. AT7519 potently inhibited the proliferation of various human tumor cell lines and this activity is cell cycle related. AT7519 was also effective in cell lines with p53 mutants or suppression, suggesting that the anti-proliferation efficacy is p53-independent. In HCT116 cells, 24 h-treatment of AT7519 resulted in a remarkable induction of G0-G1 and G2-M cell cycle arrest. Besides that, AT7519 at concentrations relating to IC50 induced cell apoptosis (24 h) in HCT116, A2780 and HT29 cells with 52%, 3% and 94% survival, respectively. Moreover, in HCT116 tumor-bearing mice, 10 mg/kg AT7519 with intraperitoneal injection caused inhibition of NPM phosphorylation and induced apoptosis [1, 2].

References:
[1] Squires M S, Feltell R E, Wallis N G, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Molecular cancer therapeutics, 2009, 8(2): 324-332.
[2] Wyatt P G, Woodhead A J, Berdini V, et al. Identification of N-(4-Piperidinyl)-4-(2, 6-dichlorobenzoylamino)-1 H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design†. Journal of medicinal chemistry, 2008, 51(16): 4986-4999.