Byl719

Manufactured by Novartis

Sourced in Switzerland

BYL719 is a laboratory research product manufactured by Novartis. It is a small-molecule inhibitor designed for use in scientific research and experiments. The core function of BYL719 is to selectively target and inhibit the activity of the PI3K protein.

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Lab products found in correlation

15 protocols using byl719

Multiparametric Western Blot Analysis

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The antibodies anti-pAKT Ser473 (#4060), anti-pAKT thr308 (#9275), anti-AKT (#4691), anti-pS6 S235/236 (#4858), anti-pS6 S240/244 (#5364), anti-S6, anti-pERK1/2 Thr202/Tyr204 (#9101), and anti-ERK1/2 (#4695) were from Cell Signaling Technology. Anti-LC3B was obtained from Sigma-Aldrich (L8918). KI67 was purchased from Vector laboratories (#VP K451). Anti-Actin was from MP Biomedicals (691001). Novartis Pharma AG (Basel, Switzerland) provided BYL719 and AEW541. LDE225, MK2206, AZD6482,AZD6738, GDC0032, PHA-665752, 17-AAG, LEE011, LY2835219, LBH589, ABT737 and Navitoclax were purchased from Selleckchem (Houston TX, USA). TUNEL- TREVIGEN, cat no-4815-30-K).

Zorea J., Prasad M., Cohen L., Li N., Schefzik R., Ghosh S., Rotblat B., Brors B, & Elkabets M. (2018). IGF1R upregulation confers resistance to isoform-specific inhibitors of PI3K in PIK3CA-driven ovarian cancer. Cell Death & Disease, 9(10), 944.

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Neuroendocrine Tumor Cell Lines Characterization

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Pancreatic neuroendocrine tumor cell lines BON-1 [39 (link)] and QGP-1 [40 (link)] (both obtained from Japanese Collection of Research Bioresources) and the typical bronchial carcinoid-NET cell line NCI-H727 (H727) [41 (link)] (purchased from ATCC, Manassas, VA) underwent authentication at the DSMZ (Braunschweig, Germany, in 2014), and their neuroendocrine features were confirmed by immunocytochemistry. Participating researchers received cell aliquots of the same passage together with SOPs for culture procedures. Cell lines had been tested for PIK3CA mutations by panel sequencing (Ion Seq Torrent Lung and Colon Panel v2). No PIK3CA mutations had been detected. BYL719 is a selective PI3Kα inhibitor developed by Novartis Pharma. All cell lines have been treated with different concentrations (10 nM– 250 μM) of BYL719 (kindly provided by Novartis) versus DMSO control for several time periods according to assay type. Everolimus was purchased from Selleckchem (Munich, Germany) and used in concentrations between 1 and 10nM.

Nölting S., Rentsch J., Freitag H., Detjen K., Briest F., Möbs M., Weissmann V., Siegmund B., Auernhammer C.J., Aristizabal Prada E.T., Lauseker M., Grossman A., Exner S., Fischer C., Grötzinger C., Schrader J, & Grabowski P. (2017). The selective PI3Kα inhibitor BYL719 as a novel therapeutic option for neuroendocrine tumors: Results from multiple cell line models. PLoS ONE, 12(8), e0182852.

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Targeted Gene Editing in Cancer Cell Lines

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Cell lines and culture media are as follows: HCT116 cells (McCoy's 5A Medium GIBCO#16600 with 10% FBS); Mel-Juso, ESS1, and NCIH1048 cells (RPMI-1640 with 10% FBS); Mel202 (RPMI-1640 with 15% FBS, from Schepens Eye Institute); Karpas422 (RPMI-1640 with 10% FBS and 1Â Glutamax from LifeTech). At low seeding density, Mel202 requires 30% conditioned medium to support cell proliferation. All lines were authenticated by SNP fingerprinting, and generally used within 20 passages. TALENs targeting p53 and SF3B1 were purchased from LifeTech. Backbone donor vector for homologous recombination was generated by gene synthesis from LifeTech. Left and right homologous recombination arms were obtained from genomic PCR and cloned into the restriction sites in the backbone donor vector (Nde1 and Xho1 for the left arm; EcoR1 and Not1 for the right arm, Xho1 site was removed in the end). Detailed information on the targeting sequences of TALENs and CRISPR as well as the donor vector design and PCR primers are provided in Supplementary Experimental Procedures. The chemical compounds used in this study are as follows: Doxorubicin (Sigma) and Nutlin-3 (Sigma); BYL719 (Novartis); El1 (Novartis); Shield-1 (Clontech). Shield-1 powder was dissolved in 100% EtOH at 1mmol/L and stored at À20 C. Shield-1 was added to the fresh tissue culture media right before usage.

Zhou Q., Derti A., Ruddy D., Rakiec D., Kao I., Lira M., Gibaja V., Chan H., Yang Y., Min J., Schlabach M.R, & Stegmeier F. (2015). A chemical genetics approach for the functional assessment of novel cancer genes. Cancer research, 75(10).

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Breast Cancer Cell Lines and Targeted Inhibitors

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The human breast cancer cell lines used in this analysis, including T47D, MDA-MB-468, BT549, HCC38, HCC1187, and Hs578T were obtained from American Type Culture Collection (Rockville, MD). MDA-MB-231 was kindly provided by Dr. Emily Wang (City of Hope). BT549, HCC38 and HCC1187 were cultured in RPMI 1640 medium (Mediatech Inc., Manassas, VA) supplemented with 10% fetal bovine serum (FBS, Atlanta Biologicals, Norcross, GA) and 1% penicillin/streptomycin. MDA-MB-468 cells were propagated in 1:1 DMEM/F12 (1:1) (Gibco, Invitrogen) supplemented with 10% FBS and 1% penicillin/streptomycin. MDA-MB-231 and Hs578T were cultured in DMEM medium (Mediatech Inc., Manassas, VA) supplemented with10% fetal bovine serum and 1% penicillin/streptomycin.
All cells were incubated at 37 °C at 5% CO₂. BYL719 (alpelisib, selective PI3K-α inhibitor) and LEE011 (ribociclib, highly specific CDK4/6 inhibitor) were obtained under a Material Transfer Agreement with Novartis (Basel, Switzerland).

Yuan Y., Wen W., Yost S.E., Xing Q., Yan J., Han E.S., Mortimer J, & Yim J.H. (2019). Combination therapy with BYL719 and LEE011 is synergistic and causes a greater suppression of p-S6 in triple negative breast cancer. Scientific Reports, 9, 7509.

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Comprehensive PI3K/mTOR Inhibitor Sourcing

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The class I PI3K inhibitor ZSTK474, the PI3K delta inhibitor IC-87114, the mammalian target of rapamycin complex (mTORC) 1/2 inhibitor AZD8055 and the mTORC1 inhibitor rapamycin were purchased from Selleckchem (Suffolk, UK). The PI3K gamma inhibitor AS-605240 was sourced from Cambridge Bioscience (Cambridge, UK). Akt inhibitor VIII was acquired from Merck chemicals (Dramstadt, Germany). The PI3K beta inhibitor GSK2636771 was obtained from Axon Medchem (Groningen, The Netherlands). The PI3K alpha inhibitor BYL719 was provided by Novartis (Basel, Switzerland).

Carter E., Miron-Buchacra G., Goldoni S., Danahay H., Westwick J., Watson M.L., Tosh D, & Ward S.G. (2014). Phosphoinositide 3-Kinase Alpha-Dependent Regulation of Branching Morphogenesis in Murine Embryonic Lung: Evidence for a Role in Determining Morphogenic Properties of FGF7. PLoS ONE, 9(12), e113555.

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Modeling Lung Cancer Progression in Mice

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Animal experiments were conducted under protocols approved by the UCSF Institutional Animal Care and Use Committee. Kras^LSL, Pik3ca^Lat-H1047R, Trp53^lox, R26^mT-mG and SPC^CreER mice were previously described (7 (link),10 (link),17 (link)–19 (link)). Adenovirus encoding Cre recombinase (Ad-CMV-Cre, Viraquest) was instilled into the nasal passages of mice as previously described (20 (link)). Tumor bearing mice were euthanized for analysis either at a pre-determined time point or when their body conditioning score (BCS) was ≤2 (21 (link)). BrdU labeling was achieved by intraperitoneal (IP) injection of 1mg BrdU (BD) dissolved in PBS. Tamoxifen (Sigma) was administered by IP injection (1mg/mouse in peanut oil) for 5 consecutive days. Orthotopic lung cancer models were generated by tail vein injection of cells in DMEM. Bioluminescence was measured using a Xenogen IVIS Spectrum system 15 minutes after injection of 150mg/kg D-luciferin (GoldBio). BYL719 (Novartis) was formulated in 0.5% Methylcellulose (Sigma) and dosed by oral gavage (p.o.) at 50mg/kg either once (q.d.) or twice (b.i.d.) per day. Kaplan-Meier survival curves were plotted using Prism and statistical significance determined using the Log-rank (Mentel-Cox) test and the Gehan-Breslow-Wilcoxon test.

Green S., Trejo C.L, & McMahon M. (2015). PIK3CAH1047R accelerates and enhances KRASG12D-driven lung tumorigenesis. Cancer research, 75(24), 5378-5391.

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PI3K Inhibitor Reconstitution and Storage

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IC-87114 (PI3Kδ inhibitor) was obtained from Selleckchem (Houston, TX; S1268) and reconstituted to maximal solubility of 2.52 mmol/L in DMSO, and aliquots were stored at −80°C. AS-605240 (PI3Kγ inhibitor) was obtained from Sigma-Aldrich (Natick, MA; A0233) and reconstituted to 9.7 mmol/L in DMSO, and aliquots were stored at −80°C. The following inhibitors were obtained from Novartis (Cambridge, MA): BKM-120 (pan PI3K), BYL-719 (PI3Kα inhibitor), and MEK-162 (MEK inhibitor). These were reconstituted in DMSO 10 mmol/L, and aliquots were stored at −20°C.

Zwang N.A., Zhang R., Germana S., Fan M.Y., Hastings W.D., Cao A, & Turka L.A. (2016). Selective Sparing of Human Tregs by Pharmacologic Inhibitors of the Phosphatidylinositol 3-Kinase and MEK Pathways. American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons, 16(9), 2624-2638.

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Inhibitor Combination Protocol

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RAD001 and the PI3K inhibitors (BEZ235, BKM120 and BYL719) were generously provided by Novartis Oncology (Basel, Swiss). Inhibitors were dissolved in dymethil sulfoxide (DMSO, Sigma- Aldrich), and the stock solutions were diluted to final concentrations in medium.

Passacantilli I., Capurso G., Archibugi L., Calabretta S., Caldarola S., Loreni F., Fave G.D, & Sette C. (2014). Combined therapy with RAD001 e BEZ235 overcomes resistance of PET immortalized cell lines to mTOR inhibition. Oncotarget, 5(14), 5381-5391.

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Combination Therapy for Cancer Cells

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Gefitinib (Selleck, China) and BYL719 (Novartis) were dissolved in dimethyl sulfoxide (DMSO) to a 20 mM concentration. DMEM/F12 medium (Cat. No.:11,330,032), B27 (Cat. No. 11,330,032), 0.25% pancreatin (Cat. No. 15,050,065) were purchased from Gibco (USA); EGF (Cat. No.: AF-100-15-100), bFGF (Cat. No. AF-100-18 C) were purchased from PeproTech Company (USA); Matrigel (Cat. No. 356,231), Cell Recovery Solution (Cat. No. 354,253) were purchased from Corning Company (U.S.); Puromycin was purchased from Mpbio Company (U.S., Cat. No. 219,453,925); Y-27,632 was purchased from AbMole (U.S., Cat. No. 129,830,382). CellTiter-Glo® 3D Cell Viability Assay was purchased from Promega (USA, Cat. No. G9682); AnnexinV-FITC/PI Apoptosis Kit was purchased from BD (USA, Cat. No. 556,547), HiScript III RT SuperMix for qPCR (+ gDNA wiper) (Cat. No. R323-01), ChamQ SYBR qPCR Master Mix (Cat. No. Q311-03) were purchased from Novozymes Biotechnology Co., Ltd. (China). The 3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) power was purchased from Sigma Aldrich (Mo, USA). 5-Ethynyl-2′-deoxyuridine (EdU) detection kit was ordered from Ribo Biological Co., Ltd. (Guangzhou, China). Antibodies to PIK3CA, AKT, p-AKT (Ser473), and GAPDH were purchased from Cell Signaling Technology (MA, USA).

Yu Y., Xiao Z., Lei C., Ma C., Ding L., Tang Q., He Y., Chen Y., Chang X., Zhu Y, & Zhang H. (2023). BYL719 reverses gefitinib-resistance induced by PI3K/AKT activation in non-small cell lung cancer cells. BMC Cancer, 23, 732.

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Establishment of BYL719-resistant Cell Lines

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All other cell lines were purchased from commercial vendors. For the entire list of cell lines see Supplemental Experimental Procedures.
CAL33R, LB771-HNCR, KYSE70R, KYSE180R cells were obtained after chronic exposure to increasing concentrations of BYL719 for ∼8 months. All cells were maintained at 37°C in a humidified atmosphere at 5% CO2. The PI3Kα inhibitor, BYL719, was kindly provided by Novartis. The AXL inhibitor R428, EGFR inhibitor erlotinib, MET inhibitor crizotinib, mTOR inhibitors RAD001 and AZD8055 and PKC inhibitors were purchased from Santa Cruz Chemicals or Selleckchem. All compounds were dissolved in dimethyl sulfoxide (DMSO) for in vitro experiments.

Elkabets M., Pazarentzos E., Juric D., Sheng Q., Pelossof R.A., Brook S., Benzaken A.O., Rodon J., Morse N., Yan J.J., Liu M., Das R., Chen Y., Tam A., Wang H., Liang J., Gurski J.M., Kerr D.A., Rosell R., Teixidó C., Huang A., Ghossein R.A., Rosen N., Bivona T.G., Scaltriti M, & Baselga J. (2015). AXL mediates resistance to PI3Kα inhibition by activating the EGFR/PKC/mTOR axis in head and neck and esophageal squamous cell carcinomas. Cancer cell, 27(4), 533-546.

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