| Identification | Back Directory | [Name]
AT-7519 trifluoroacetate | [CAS]
1431697-85-6 | [Synonyms]
AT7519 TFA
AT7519 TFA,AT-7519 TFA
AT 7519 trifluoroacetate
AT-7519 trifluoroacetate
AT7519 (trifluoroacetate)
AT 7519 TRIFLUOROACETATE;AT-7519 TRIFLUOROACETATE
4-[(2,6-Dichlorobenzoyl)amino]-N-4-piperidinyl-1H-pyrazole-3-carboxamide 2,2,2-trifluoroacetate | [Molecular Formula]
C18H18Cl2F3N5O4 | [MOL File]
1431697-85-6.mol | [Molecular Weight]
496.268 |
| Hazard Information | Back Directory | [Uses]
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. | [in vivo]
AT7519 TFA inhibits tumor growth in a human MM xenograft mouse model[1]. AT7519 (4.6 and 9.1 mg/kg/dose) inhibits the growth of early-stage HCT116 tumor xenografts. AT7519 (10 mg/kg, i.p.) TFA also inhibits the target CDKs in HCT116 tumor-bearing BALB/c nude mice[2]. | [IC 50]
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) | [storage]
Store at -20°C | [References]
[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 |
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