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Alpelisib

Manufactured by Selleck Chemicals
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Alpelisib is a lab equipment product manufactured by Selleck Chemicals. It is a phosphoinositide 3-kinase (PI3K) inhibitor. Alpelisib is used for research purposes.

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Lab products found in correlation

Trametinib, by Selleck Chemicals (5 mentions) Mk2206, by Merck Group (2 mentions) Trametinib, by GlaxoSmithKline (2 mentions) Fulvestrant, by Selleck Chemicals (2 mentions) Bi d1870, by Selleck Chemicals (2 mentions) Dimethyl sulfoxide (dmso), by Merck Group (2 mentions) Cmc na, by Sinopharm (2 mentions) Tween 80, by Sangon (2 mentions) Pictilisib, by Selleck Chemicals (2 mentions) Azd8186, by Selleck Chemicals (2 mentions) Ly294002, by Selleck Chemicals (2 mentions) Everolimus, by Selleck Chemicals (2 mentions) Sphingosine 1 phosphate (s1p), by Cayman Chemical (1 mentions) Tgf β neutralizing antibody, by BioXCell (1 mentions) Galunisertib, by Selleck Chemicals (1 mentions) Ars 1620, by MedChemExpress (1 mentions) Lmk 235, by MedChemExpress (1 mentions) Rs 504393, by Cayman Chemical (1 mentions) Rmil 6, by Thermo Fisher Scientific (1 mentions) Pgf2α, by Cayman Chemical (1 mentions)

Spelling variants of this product

Alpelisib (BYL719), (6 citations)

21 protocols using alpelisib

1

Pharmacological Modulation of Signaling Pathways

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For in vitro studies: PGF2α (Cayman), rmFGF1 (Peprotech), rmPDGFBB (Peprotech), rmPDGFAA (Peprotech), rh/mWnt-5a (R&D), LPA (Santa Cruz biotech), rmIL6 (Peprotech), S1P (Cayman), Adapalene (Selleckchem), SAG (Tocris), rmTGFβ1(R&D), rmTGFβ2(R&D), rmTGFβ3 (R&D), CCL2 (BioLegend), CCR2 inhibitor (Santa Cruz Biotechnology), MEKi (PD0324901, 2 μM, Selleckchem), PI3Ki (LY294002, 2 μM, Selleckchem) , mTORi (Rapamycin, 100 nM, Selleckchem), Trametinib (Selleckchem, 50 nM), Alpelisib (Selleckchem, 5 μM) and ARS-1620 (MedChemExpress).
For in vivo studies: TGFβ neutralizing antibody (BioXCell, Clone 1D11, 200 μg, every other day, i.p), Clodronate liposome (Liposoma, 0.1 ml per 10 mg weight, every 5 days, i.p), Trametinib (Selleckchem, 0.3 or 1 or 3 mg/kg as indicated, q.d., oral), Alpelisib (Selleckchem, 50 mg/kg, once per day, oral), ARS-1620 (MedChemExpress, 200 mg/kg, q.d., oral), LMK-235 (MedChemExpress, 5 mg/kg, q.d., i.p.), Galunisertib (Selleckchem, 50 mg/kg, b.i.d., oral), mouse CCL2 neutralizing antibody (BioXCell, 5 mg/kg, every 2 days, i.p.), and RS 504393 (Cayman, 2 mg/kg, q.d., i.p.).
Hou P., Kapoor A., Zhang Q., Li J., Wu C.J., Li J., Lan Z., Tang M., Ma X., Ackroyd J.J., Kalluri R., Zhang J., Jiang S., Spring D.J., Wang Y.A, & DePinho R.A. (2020). Tumor microenvironment remodeling enables bypass of oncogenic KRAS dependency in pancreatic cancer. Cancer discovery, 10(7), 1058-1077.
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2

Cell Growth Inhibition Assay with Kinase Inhibitors

Cited 1 time
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Trametinib (GSK1120212, Tram) was kindly provided by GlaxoSmithKline (Brentford, Middlesex, UK). Alpelisib (BYL719, Alp), dactolisib (BEZ235, Dact), and Geda (PF05212384) were purchased from Selleck Chemicals (Huston, TX, USA). MK-2206 (MK) was kindly provided by Merck and Co. (Kenilworth, NJ, USA). Alp, Geda, MK, and Tram were dissolved in DMSO as a 1 mM (Geda, MK and Tram) and 5mM (Alp) stock solution, dact was dissolved in DMF as a 1mM. All the drugs were stored at -20°C (Alp, Dact, MK, and Tram) or -80°C (Geda). Eve (RAD001) was kindly provided from Novartis Pharma (Basel, Switzerland) and was dissolved in 100% ethanol as a 10 mM stock solution and stored at -20°C.
The final concentration of drugs was obtained by dilution with culture medium.
Effects on cell growth after 72 h of different treatments were monitored by Crystal Violet assay, as previously described (10 (link)).
Conciatori F., Salvati E., Ciuffreda L., Shirasawa S., Falcone I., Cognetti F., Ferretti G., Zeuli M., Del Bufalo D., Bazzichetto C, & Milella M. (2022). Fibroblast-Induced Paradoxical PI3K Pathway Activation in PTEN-Competent Colorectal Cancer: Implications for Therapeutic PI3K/mTOR Inhibition. Frontiers in Oncology, 12, 862806.
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3

Selective Inhibition of SYK/PI3K Pathway

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Selective small molecule inhibitors specifically against the SYK/PI3K signaling pathway were investigated (108 (link)). For repurposing purpose, only approved or investigational compounds in phase-III clinical trials were used in the screening assay. All inhibitors (dexamethasone [D1756; Merck], entospletinib [S7523; Selleckchem], R406 [S1533; Selleckchem], alpelisib [S2814; Selleckchem], idelalisib [HY-13026; MedChemExpress], duvelisib [HY-17044; MedChemExpress], were purchased in powdered form and dissolved according to the distributor’s instructions). Macrophages were preincubated with inhibitors (or DMSO as a control) for 30 min at 37°C. After preincubation, macrophages were stimulated with 20 μg/ml polyinosinic:polycytidylic acid (poly(I:C), Sigma-Aldrich) and seeded in a density of 50,000 cells/well in pre-coated 96-well plates in 200 μl/well medium.
Geyer C.E., Chen H.J., Bye A.P., Manz X.D., Guerra D., Caniels T.G., Bijl T.P., Griffith G.R., Hoepel W., de Taeye S.W., Veth J., Vlaar A.P., Vidarsson G., Bogaard H.J., Aman J., Gibbins J.M., van Gils M.J., de Winther M.P, & den Dunnen J. (2023). Identification of new drugs to counteract anti-spike IgG-induced hyperinflammation in severe COVID-19. Life Science Alliance, 6(11), e202302106.
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4

Proliferation Assay with Alpelisib and Rapamycin

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For proliferation assays, cells were seeded at a density of 3000 cells/well (24 h) or 1500 cells/well (48–144 h) on 96-well plates and treated with different concentrations of alpelisib and/or rapamycin (both Selleckchem, Munich, Germany). Medium was replaced every 72 h. Cell viability measures were performed using the Cell Proliferation Reagent WST-1 (Roche Diagnostics GmbH, Mannheim, Germany) according to the manufacturer’s protocol. After WST-1 assay, cells were fixed and nuclei were stained with Hoechst 33342 (Sigma, Munich, Germany) for 5 min at a concentration of 10 µg/ml in DPBS. Hoechst fluorescence was detected at 455 nm.
Kirstein A.S., Augustin A., Penke M., Cea M., Körner A., Kiess W, & Garten A. (2019). The Novel Phosphatidylinositol-3-Kinase (PI3K) Inhibitor Alpelisib Effectively Inhibits Growth of PTEN-Haploinsufficient Lipoma Cells. Cancers, 11(10), 1586.
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5

Preparation of Drug Stock Solutions

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Trametinib (GSK1120212) and dabrafenib (GSK2118436) were kindly provided by GlaxoSmithKline (Brentford, Middlesex, UK). Gedatolisib (PF05212384) was kindly provided by Pfizer Inc. (New York, NY, USA). SCH772984 and alpelisib were purchased by Selleckchem (Houston, TX, USA). Everolimus was obtained from Novartis Pharma (Basel, Switzerland). MK-2206 was kindly provided by Merck and Co. (Kenilworth, NJ, USA).
Trametinib, dabrafenib, SCH772984, alpelisib and MK-2206 were dissolved in DMSO as 1 mM, 10 mM, 0.2 mM, 10 mM and 1 mM stock solution, respectively and stored at −20 °C. Gedatolisib was dissolved in DMSO as 1 mM stock solution and stored at −80 °C. Everolimus was dissolved in 100% ethanol as a 10 mM stock solution and stored at −20 °C.
The final concentration of drugs was obtained by dilution with culture medium.
Conciatori F., Bazzichetto C., Amoreo C.A., Sperduti I., Donzelli S., Diodoro M.G., Buglioni S., Falcone I., Shirasawa S., Blandino G., Ferretti G., Cognetti F., Milella M, & Ciuffreda L. (2020). BRAF status modulates Interelukin-8 expression through a CHOP-dependent mechanism in colorectal cancer. Communications Biology, 3, 546.
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6

PIK3CA Mutant OSCC Cell Lines

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A total of three human OSCC cell lines, SAS (wild-type PIK3CA gene), HSC-2 and HSC-3 (both with mutant PIK3CA gene) were used in the present study, as found in a previous study (12 (link)) and were cultured in a 1:1 mixture of Ham's F-12/Dulbecco's modified Eagle's medium supplemented with 10% fetal bovine serum (all Trace Scientific, Ltd; Thermo Fisher Scientific, Inc.). All cells were maintained at 37°C in a humidified incubator with 5% CO2 and 19% O2. Alpelisib, a selective PI3Kα inhibitor, was purchased from Selleck Chemicals (cat. no. BS119QD), dissolved in dimethyl sulfoxide (DMSO), and adjusted to a range of concentrations (0.1–100 µM) with culture medium (1:1 mixture of Ham's F-12 and DMEM supplemented with 10% fetal bovine serum) (all Trace Scientific, Ltd; Thermo Fisher Scientific, Inc.). Cetuximab (cat. no. C225) was purchased from Merck KGaA. Working solutions were freshly prepared from the stock solution by diluting with cell culture medium on the day of the experiment.
Tsuchihashi H., Naruse T., Yanamoto S., Okuyama K., Furukawa K., Omori K, & Umeda M. (2020). Selective inhibition of PI3K110α as a novel therapeutic strategy for cetuximab-resistant oral squamous cell carcinoma. Oncology Reports, 44(3), 863-872.
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7

Cell Viability Assay with Targeted Inhibitors

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Cells were plated in 50μL of media at 9,000 cells/well in 2D and ULA (Corning #3474) 96-well plates. Treatments were added 24 hours post seeding in an additional 50μL of respective media. IGF1R inhibitors BMS-754807 (Selleckchem #S1124) and OSI-906 (Selleckchem #S1091), PI3K inhibitor Alpelisib (Selleckchem #S2814), Akt inhibitor MK-2206 (Selleckchem #S1078), MEK inhibitor U0126 (Selleckchem #S1102) and Fulvestrant (Selleckchem #S1191) were dissolved in DMSO with a final ≤0.5% DMSO concentration in treatments. Plates were collected at day 6 and measured by CellTiter-Glo (Promega #PR-G7573) following the manufacturer’s protocol. Cell viability values were analyzed following blank cell deductions and normalization to vehicle readings. IC50 values for viability were calculated by nonlinear regression and statistical differences evaluated using sum-of-squares Global f-test (p<0.05). Synergy was assessed using SynergyFinder (35 (link)).
Elangovan A., Hooda J., Savariau L., Puthanmadhomnarayanan S., Yates M.E., Chen J., Brown D.D., McAuliffe P.F., Oesterreich S., Atkinson J.M, & Lee A.V. (2022). Loss of E-cadherin Induces IGF1R Activation and Reveals a Targetable Pathway in Invasive Lobular Breast Carcinoma. Molecular cancer research : MCR, 20(9), 1405-1419.
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8

Evaluation of Candidate Inhibitors

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YM-254890 was purchased from Focus Biomolecules (10–1590) and Wako Pure Chemical Industries (257–00631). Linsitinib (OSI-906) was purchased from Selleck Chemical (S1091) and LC Laboratories (L-5814). Picropodophyllin (PPP) and Alpelisib (BYL719) were purchased from Selleck Chemical. IGF1 was purchased from Abcam.
Lapadula D., Lam B., Terai M., Sugase T., Tanaka R., Farias E., Kadamb R., Lopez-Anton M., Heine C.C., Modasia B., Aguirre-Ghiso J.A., Aplin A.E., Sato T, & Benovic J.L. (2023). IGF1R inhibition enhances the therapeutic effects of Gq/11 inhibition in metastatic uveal melanoma progression. Molecular cancer therapeutics, 22(1), 63-74.
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9

Compound Preparation and Solvents

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CYH33 was provided by Shanghai HaiHe Pharmaceutical Co. Ltd. Alpelisib, GSK21118436, MEK162, GDC0994, BI-D1870, RAD001, and OTX015 were purchased from Selleck Chemicals (Houston, TX, USA). For in vitro experiments, all compounds were dissolved in dimethyl sulfoxide (DMSO, Sigma, St. Louis, MO, USA) at the concentrations of 10 mM and stored at −20 oC. For in vivo studies, CYH33 and MEK162 were solved in normal saline containing 0.5% Tween 80 (v/v; Sangon Biotech, Shanghai, China), and 1% CMC-Na (m/v; SINOPHARM, Beijing, China).
Wang Y.X., Zhang X., Ma Q.Y., Hu L.D., Zhang X., Wang Y., Xu L., Yang C.H., Tan C., Kong X.Y., Ding J, & Meng L.H. (2021). Adaptive resistance to PI3Kα-selective inhibitor CYH33 is mediated by genomic and transcriptomic alterations in ESCC cells. Cell Death & Disease, 12(1), 85.
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10

Evaluation of Targeted Cancer Inhibitors

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Tipifarnib (RR11577), AZD8186 (S7694), Alpelisib (BYL719; S2814), and Pictilisib (GDC-0941, S1065) were purchased from SelleckChem.
Nigam A., Krishnamoorthy G., Chatila W., Berman K., Saqcena M., Walch H., Ho A., Schultz N., Fagin J, & Untch B. (2023). Cooperative Genomic Lesions in HRAS-Mutant Cancers Predict Resistance to Farnesyltransferase Inhibitors. Research Square.
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