Nilotinib

Manufactured by Novartis

Sourced in Switzerland, United States

Nilotinib is a tyrosine kinase inhibitor used as a laboratory tool for research purposes. It functions by inhibiting the Bcr-Abl protein, which is associated with certain types of leukemia. The specific intended use and applications of Nilotinib should be determined by the researcher based on their study requirements.

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Lab products found in correlation

Imatinib, by Novartis (24 mentions) Dasatinib, by Bristol-Myers Squibb (8 mentions) Ponatinib, by MedKoo Biosciences (3 mentions) Sb225002, by Selleck Chemicals (2 mentions) Imatinib mesylate, by Novartis (2 mentions) Dasatinib, by Novartis (2 mentions) Dimethyl sulfoxide (dmso), by Merck Group (2 mentions) Asciminib, by Novartis (2 mentions) Ponatinib, by Selleck Chemicals (2 mentions) Glutamine, by Merck Group (2 mentions) Streptomycin, by Merck Group (2 mentions) Cumate, by System Biosciences (2 mentions) Plx4720, by Selleck Chemicals (2 mentions) Mk2206, by MedChemExpress (2 mentions) Isopropyl β d 1 thiogalactopyranoside (iptg), by Thermo Fisher Scientific (2 mentions) Gnf 2 gnf 5, by Selleck Chemicals (2 mentions) Su6656, by Merck Group (2 mentions) Mk 2206, by Selleck Chemicals (2 mentions) Sch772984, by Selleck Chemicals (2 mentions) Penicillin streptomycin mix, by Merck Group (2 mentions)

45 protocols using nilotinib

Nilotinib and Imatinib Effects on NF1 Schwann Cells

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The donor of the study specimen was a 12-year-old female NF1 patient, diagnosed according to the modified National Institutes of Health criteria [18] (link). A parent of the patient gave informed written consent in addition to assent from the patient. The Institutional Review Board approved the study (OB-061/05). Her PNF was operated at the Department of Maxillofacial Surgery, University Hospital Hamburg-Eppendorf. A part of the tumor was kept in Hanks buffered saline and delivered into the laboratory for cell culture and for xenografting. Schwann cells from the PNF were cultured and identified as previously described [16] (link).
After ensuring purity of 85%, PNF-derived Schwann cells were treated with nilotinib and imatinib (Novartis Pharma AG, Switzerland), each at 0, 5, 10, 15 and 20 µM for 10 days. Cell proliferation and viability assays were performed as previously described [16] (link).

Wei J., Freytag M., Schober Y., Nockher W.A., Mautner V.F., Friedrich R.E., Manley P.W., Kluwe L, & Kurtz A. (2014). Nilotinib Is More Potent than Imatinib for Treating Plexiform Neurofibroma In Vitro and In Vivo. PLoS ONE, 9(10), e107760.

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Dual inhibition of Nilotinib and CXCR2 in TNFα signaling

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Nilotinib (TKI) supplied by Novartis Pharmaceuticals, and CXCR2 inhibitor (SB225002) purchased from Selleckchem (cat no. S7651, Houston, TX) were stored in 10mM dimethylsulfoxide (DMSO) at 20°C. Recombinant mouse TNFα (animal-free, clone MP6-XT22, cat. no. 718004, BioLegend, San Diego, CA) was reconstituted in water and stored at −20°C. Undiluted TNFα neutralizing antibody (InVivoMAb anti-mouse TNFα, clone XT3.11, cat no. BE0058, BioXCell, West Lebanon, NH) was stored at 4°C, and reconstituted in InVivoPure pH 8.0 dilution buffer just before use.

Agarwal P., Li H., Choi K., Hueneman K., He J., Welner R.S., Starczynowski D.T, & Bhatia R. (2021). TNF-α-induced alterations in stromal progenitors enhance leukemic stem cell growth via CXCR2 signaling. Cell reports, 36(2), 109386.

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Dual inhibition of Nilotinib and CXCR2 in TNFα signaling

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Drug Preparation and Dissolution

Cited 2 times

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JQ1 and iBET were synthesized as described (15 (link), 17 (link)). Imatinib and nilotinib were from Novartis Pharma (Basel, Switzerland). Jak Inhibitor 1 was obtained from EMD Millipore (Billerica, MA). All drugs were dissolved in dimethyl sulfoxide (DMSO) and were diluted to a final concentration of 0.1% DMSO in all experiments.

Liu S., Walker S.R., Nelson E.A., Cerulli R., Xiang M., Toniolo P.A., Qi J., Stone R.M., Wadleigh M., Bradner J.E, & Frank D.A. (2014). Targeting STAT5 in Hematological Malignancies through Inhibition of the Bromodomain and Extra-Terminal (BET) Bromodomain Protein BRD2. Molecular cancer therapeutics, 13(5), 1194-1205.

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Imatinib, Nilotinib, and Carfilzomib Reconstitution

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Imatinib and nilotinib were provided by Novartis Pharmaceuticals (Surrey, UK) and reconstituted in sterile water or DMSO, respectively. Carfilzomib was provided by Onyx Pharmaceuticals, Inc (South San Francisco, CA, USA) and was reconstituted in DMSO.

Crawford L.J., Chan E.T., Aujay M., Holyoake T.L., Melo J.V., Jorgensen H.G., Suresh S., Walker B, & Irvine A.E. (2014). Synergistic effects of proteasome inhibitor carfilzomib in combination with tyrosine kinase inhibitors in imatinib-sensitive and -resistant chronic myeloid leukemia models. Oncogenesis, 3(3), e90-.

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Cell Culture Media and Reagents

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Minimum essential media (MEM), minimum essential media α modification (αMEM), and Dulbecco’s minimum essential media (DMEM) powder, Opti-MEM^®, sodium pyruvate (NaP), fetal bovine serum (FBS) and Penicillin/Streptomycin mixture (10,000U/mL) were purchased from Gibco BRL (ThermoFisher Scientific, Waltham, MA). L-ascorbic acid-2-phosphate (AA2P), bosutinib and puromycin dihydrochloride were purchased from Sigma-Aldrich Co. (St. Louis, MO). Imatinib mesylate and nilotinib were supplied by Novartis Pharma AG (Basel, Switzerland). Rat PDGF-BB was purchased from R&D Systems (Minneapolis, MN). Polybrene was purchased from Santa Cruz Biotechnology (Dallas, TX). Lipofectamine^® 2000 Transfection Reagent was purchased from Life Technologies (ThermoFisher Scientific).

O’Sullivan S., Tay M.L., Lin J.M., Bava U., Callon K., Cornish J., Naot D, & Grey A. (2016). Tyrosine Kinase Inhibitors Regulate OPG through Inhibition of PDGFRβ. PLoS ONE, 11(10), e0164727.

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Kinase Inhibitors and Autophagy

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Imatinib and nilotinib were obtained from Novartis. Chloroquine, GNF-2, and GNF-5 were purchased from Sigma-Aldrich. 3-Methyladenine was purchased from R&D systems. Lysotracker Red was purchased from Lonza. Interleukine-3 was purchased from Calbiochem.

Fu D., Zhou J., Zhu W.S., Manley P.W., Wang Y.K., Hood T., Wylie A, & Xie X.S. (2014). Imaging the Intracellular Distribution of Tyrosine Kinase Inhibitors in Living Cells with Quantitative Hyperspectral Stimulated Raman Scattering. Nature chemistry, 6(7), 614-622.

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Tamoxifen, Nilotinib, and SCF Modulate Ubc-Scf Signaling

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Tamoxifen (75 mg/kg, Cayman Chemical) in corn oil was administered intraperitoneally for 5 days to Ubc-SCF^Δ/Δ-cre mice. Nilotinib (50 mg/kg/day in 0.5% methylcellulose + 0.5% Tween-80, Novartis) was administered by oral gavage. SCF (100 μg/kg, PeproTech) was administered intraperitoneally for 2 weeks. For in vitro analysis, cells were cultured with 5 μM Nilotinib, 10 ng/mL SCF, or combination, for 7 days.

Shah M., Kumar H., Qiu S., Li H., Harris M., He J., Abraham A., Crossman D.K., Paterson A., Welner R.S, & Bhatia R. (2023). Low c-Kit expression identifies primitive, therapy-resistant CML stem cells. JCI Insight, 8(1), e157421.

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Combination treatment of IM and nilotinib

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IM and nilotinib were provided by Novartis International AG (Basel, Switzerland). DAC was purchased from Sigma-Aldrich (Merck KGaA, Darmstadt, Germany). The Cell Counting kit-8 (CCK-8) was purchased from Dojindo Molecular Technologies, Inc. (Kumamoto, Japan).

Jiang L.C, & Luo J.M. (2017). Role and mechanism of decitabine combined with tyrosine kinase inhibitors in advanced chronic myeloid leukemia cells. Oncology Letters, 14(2), 1295-1302.

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High-grade Glioma Cell Culture Assay

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For high-grade glioma primary cell cultures treatment assays, cells were passaged and plated in a 96-well plate at 2,000 cells/well in triplicate per condition. At 24 hours, cells were treated with chemotherapeutic agents, siRNA, or control, and assessed for viability 72 hours later using the Cell Titer Glo Assay (Promega) [28 (link)]. ON-TARGET PLUS siRNAs (GE Healthcare Dharmacon) against PDGFRA (J003162-11; J003162-12) and FGF2 (J006695-05; J006695-06) were used according to manufacturer's protocol. Chemotherapy was administered at a range of concentrations (0.01-1000 μM) based on previously published data: temozolomide (Sigma), CCNU (Sigma), Suberanilohydroxamic acid (SAHA), imatinib (Novartis), nilotinib (Novartis), and dasatinib (Bristol-Myers Squibb). Dose response curves were plotted using GraphPad Software, and IC₅₀ was calculated as the dose at which there was a 50% reduction in cell proliferation form untreated cells.

Koschmann C., Zamler D., MacKay A., Robinson D., Wu Y.M., Doherty R., Marini B., Tran D., Garton H., Muraszko K., Robertson P., Leonard M., Zhao L., Bixby D., Peterson L., Camelo-Piragua S., Jones C., Mody R., Lowenstein P.R, & Castro M.G. (2016). Characterizing and targeting PDGFRA alterations in pediatric high-grade glioma. Oncotarget, 7(40), 65696-65706.

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