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AT7519 hydrochloride

Cat. No. M3687
AT7519 hydrochloride Structure
Synonym:

AT7519 HCl

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 55  USD55 In stock
5mg USD 58  USD58 In stock
10mg USD 90  USD90 In stock
50mg USD 190  USD190 In stock
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Quality Control & Documentation
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 (for reference only)
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.
Chemical Information
Molecular Weight 418.71
Formula C16H18Cl3N5O2
CAS Number 902135-91-5
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Alessandri, et al. PLoS One. Induction of eosinophil apoptosis by the cyclin-dependent kinase inhibitor AT7519 promotes the resolution of eosinophil-dominant allergic inflammation.

[2] Mahadevan, et al. Ann Oncol. A phase I pharmacokinetic and pharmacodynamic study of AT7519, a cyclin-dependent kinase inhibitor in patients with refractory solid tumors.

[3] Squires, et al. Mol Cancer Ther. AT7519, a cyclin-dependent kinase inhibitor, exerts its effects by transcriptional inhibition in leukemia cell lines and patient samples.

[4] Santo, et al. Oncogene. AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition.

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  Catalog
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Keywords: AT7519 hydrochloride, AT7519 HCl supplier, CDK, inhibitors, activators


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