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AT7519 hydrochloride

Cat. No. M3687
AT7519 hydrochloride Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 80 In stock
10mg USD 125 In stock
50mg USD 440 In stock
100mg USD 680 In stock
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Quality Control
Biological Activity

AT7519 hydrochloride is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. AT7519 displays potent cytotoxicity and apoptosis; associated with in vivo tumor growth inhibition and prolonged survival. At the molecular level, AT7519 inhibited RNA polymerase II (RNA pol II) phosphorylation, a CDK9, 7 substrate, associated with decreased RNA synthesis confirmed by [(3)H] Uridine incorporation. In addition, AT7519 inhibited glycogen synthase kinase 3beta (GSK-3beta) phosphorylation.

Protocol
Cell Experiment
Cell lines MM.1S, MM.1R, RPMI8226, U266, RPMI8266, RPMI-Dox40, OPM1 cells, primary MM cells and PBMNCs
Preparation method Incubating cells with different concentrations of AT7519 for 24 or 48 hours at 37°C. Assaying cell viability by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrasodium bromide (MTT) dye absorbance. Measuring DNA synthesis by tritiated thymidine uptake (3H-TdR).Assessing Apoptosis by using Annexin V/PI staining. Defining the percentage of cells undergoing apoptosis as the sum of early apoptosis (Annexin V-positive cells) and late apoptosis (Annexin V-positive and PI-positive cells
Concentrations Dissolved in DMSO at a concentration of 10 mM, final concentrations 0.25-4 μM
Incubation time 24 or 48 hoursMale SCID mice inoculated subcutaneously with MM.1S cells
Animal Experiment
Animal models
Formulation Dissolved in 0.9% saline
Dosages 15 mg/kg/day
Administration Dosed i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 418.71
Formula C16H18Cl3N5O2
CAS Number 902135-91-5
Purity >99%
Solubility DMSO
Storage at -20°C
References

Induction of eosinophil apoptosis by the cyclin-dependent kinase inhibitor AT7519 promotes the resolution of eosinophil-dominant allergic inflammation.
Alessandri, et al. PLoS One. 2011;6(9):e25683. PMID: 21984938.

A phase I pharmacokinetic and pharmacodynamic study of AT7519, a cyclin-dependent kinase inhibitor in patients with refractory solid tumors.
Mahadevan, et al. Ann Oncol. 2011 Sep;22(9):2137-43. PMID: 21325451.

AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples.
Squires, et al. Mol Cancer Ther. 2010 Apr;9(4):920-8. PMID: 20354122.

AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition.
Santo, et al. Oncogene. 2010 Apr 22;29(16):2325-36. PMID: 20101221.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AT7519 hydrochloride supplier, CDK, inhibitors

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