Apitolisib

Manufactured by Genentech

Apitolisib is a lab equipment product designed for cell and molecular biology research. It is a kinase inhibitor that targets the phosphoinositide 3-kinase (PI3K) pathway. The core function of Apitolisib is to inhibit the activity of PI3K enzymes, which play a key role in cellular processes such as cell growth, proliferation, and survival.

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Lab products found in correlation

Dactolisib, by Selleck Chemicals (1 mentions) Recombinant human hgf, by R&D Systems (1 mentions) Dimethyl sulfoxide (dmso), by Merck Group (1 mentions)

2 protocols using apitolisib

Cell Line Characterization and Drug Treatments

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H460, A549 and H1975 cell lines were purchased from the European Culture and Tissue Collection. Apitolisib (GDC-0980) was gifted under a material transfer agreement from Genentech for use in this study, and was dissolved in dimethyl sulphoxide (DMSO), aliquoted and stored at −20 °C. Dactolisib (BEZ235) was purchased from Selleckchem, dissolved in DMSO, aliquoted and stored at −20 °C.

Heavey S., Dowling P., Moore G., Barr M.P., Kelly N., Maher S.G., Cuffe S., Finn S.P., O’Byrne K.J, & Gately K. (2018). Development and characterisation of a panel of phosphatidylinositide 3-kinase – mammalian target of rapamycin inhibitor resistant lung cancer cell lines. Scientific Reports, 8, 1652.

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Monoclonal Anti-MET Antibody and Kinase Inhibitors

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Onartuzumab (METMAb), a monovalent, humanized, anti-MET monoclonal antibody (Genentech, South San Francisco, CA; ref. 32 (link)), was used following the manufacturer’s instructions. For in vivo studies, onartuzumab (10 mg/kg, intraperitoneal injection) was administered twice weekly. MET tyrosine kinase inhibitor (TKI) tepotinib [EMD1214063; ref. 33 (link); EMD Serono, Rockland, MA), PI3Kα/δ TKI pictilisib [GDC-0941; ref. 34 (link); Genentech) and class 1 PI3K/mTOR TKI apitolisib [GDC-0980; ref. 34 (link); Genentech) were dissolved in dimethyl sulfoxide (DMSO) (Sigma-Aldrich, St. Louis, MO) and stored at −20°C. The stocked solution was further diluted to an appropriate final concentration upon use. For in vitro studies, DMSO in the final solution was 0.1% (v/v). For in vivo use, pictilisib at 100 mg/kg (in 100 μl of 5% DMSO) was given daily by oral gavage. All drugs were provided by the companies. Human recombinant HGF was purchased from R&D Systems (Minneapolis, MN).

Liu S., Li S., Wang B., Liu W., Gagea M., Chen H., Sohn J., Parinyanitikul N., Primeau T., Do K.A., Vande Woude G.F., Mendelsohn J., Ueno N.T., Mills G.B., Tripathy D, & Gonzalez-Angulo A.M. (2018). Cooperative effect of oncogenic MET and PIK3CA in an HGF-dominant environment in breast cancer. Molecular cancer therapeutics, 18(2), 399-412.

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