Avapritinib

Manufactured by Selleck Chemicals

Sourced in United States

Avapritinib is a selective inhibitor of the platelet-derived growth factor receptor alpha (PDGFRA) protein. It is used in laboratory research applications.

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Lab products found in correlation

3 protocols using avapritinib

Cell Viability Quantification by Luminescence

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To determine cell viability, cells were seeded in 96 well plates at a density of 4 × 10³ cells per well. After a recovery time of 24 h, the cells were exposed to diverse compounds at different drug concentrations in triplicates. The small molecule inhibitors ponatinib, nintedanib, AZD-4547, dovitinib, erdafitinib, avapritinib, and dasatinib were purchased from Selleck Chemicals (Houston, TX, USA). Upon 72 h incubation, cell survival was determined with the commercially available CellTiter-Glo^® Luminescent Cell Viability Assay (Promega, Madison, WI, USA) according to manufacturer’s instructions and luminescence signals were measured with the Tecan infinite 200Pro (Zurich, Switzerland). Dose–response curves were generated and anti-cancer activity was expressed as IC₅₀ values calculated by GraphPad Prism 8.0.1 (GraphPad Software, La Jolla, CA, USA) using point-to-point function.

Lötsch D., Kirchhofer D., Englinger B., Jiang L., Okonechnikov K., Senfter D., Laemmerer A., Gabler L., Pirker C., Donson A.M., Bannauer P., Korbel P., Jaunecker C.N., Hübner J.M., Mayr L., Madlener S., Schmook M.T., Ricken G., Maaß K., Grusch M., Holzmann K., Grasl-Kraupp B., Spiegl-Kreinecker S., Hsu J., Dorfer C., Rössler K., Azizi A.A., Foreman N.K., Peyrl A., Haberler C., Czech T., Slavc I., Filbin M.G., Pajtler K.W., Kool M., Berger W, & Gojo J. (2021). Targeting fibroblast growth factor receptors to combat aggressive ependymoma. Acta Neuropathologica, 142(2), 339-360.

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Kinase Inhibitor Screening in AML

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AML cell lines, AML, and AMKL patient cells were plated in 96-well plates (2.10⁵ cells per well) in their respective media and treated with kinase inhibitors axitinib, amumavatinib, telatinib, avapritinib, and imatinib (all from Selleckchem). Cell viability was measured after 96 hours of treatment as adenosine triphosphate (ATP) luminescence signal readout using CellTiter-Glo Assay (Promega) according to the manufacturer’s instructions.

Benbarche S., Lopez C.K., Salataj E., Aid Z., Thirant C., Laiguillon M.C., Lecourt S., Belloucif Y., Vaganay C., Antonini M., Hu J., da Silva Babinet A., Ndiaye-Lobry D., Pardieu B., Petit A., Puissant A., Chaumeil J., Mercher T, & Lobry C. (2022). Screening of ETO2-GLIS2–induced Super Enhancers identifies targetable cooperative dependencies in acute megakaryoblastic leukemia. Science Advances, 8(6), eabg9455.

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In vivo and in vitro drug administration

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For in vivo experiments, avapritinib (SelleckChem and Blueprint Medicines, Cambridge, MA) was dissolved in 0.5% carboxymethyl cellulose and 1% Tween 80 and administered by daily gavage. Imatinib was dissolved in water and administered in the drinking water as before (35 (link)). ML-7 (SelleckChem) was diluted in DMSO at 50 mg/ml and then diluted to 1 mg/ml in 30% PEG 400, 1% Tween 80. For cell culture experiments, avapritinib and ML7 were dissolved in DMSO, imatinib was dissolved in water. Experiments were performed in complete media (10% FBS) in a final concentration of 0.4% DMSO.

Azad A.K., Sirakova T.D., Rogers L.M, & Kolattukudy P.E. (1996). Targeted replacement of the mycocerosic acid synthase gene in Mycobacterium bovis BCG produces a mutant that lacks mycosides.. Proceedings of the National Academy of Sciences of the United States of America, 93(10), 4787-4792.

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