Ibrutinib

Manufactured by Merck Group

Sourced in United States

Ibrutinib is an oral medication that acts as a tyrosine kinase inhibitor. It is designed to target and inhibit the Bruton's tyrosine kinase (BTK) enzyme, which plays a key role in the B-cell receptor signaling pathway.

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12 protocols using ibrutinib

Establishing Preclinical CLL Models

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PDX models were established in 6-12 week old, male and female, NOD/Shi-SCID/IL-2Rγc^tm1sug/Jic (NOG), Mus musculus Linnaeus, 1758 (mouse) strain animals (in-house) as previously described [43 (link), 44 (link)].
Ibrutinib (Seleckchem; S2680) was resuspended in 1% methylcellulose and 0.4% Cremephor EL (Sigma; M0262 and C5135), and administered daily for 9 days by oral gavage at 12.5mg/kg, a dose which is sufficient to ensure 90% occupancy of Bruton tyrosine kinase (BTK) [45 (link)]. Rituximab (40mg/kg; Roche; 2530376), or saline control was given intravenously 3 times per week.[46 (link)] Fludarabine (0.625mg/kg, TEVA; 231-10-04151) and cyclophosphamide (6.25mg/kg, Baxter; 1001995501) or saline (control) were injected intraperitoneally 3 times per week, for two weeks, [47 (link)] whereas chlorambucil (5mg/kg; Sigma; CO253) or 3% dimethyl sulfoxide (DMSO, Sigma; D2650) vehicle control was administered daily for 5 days intraperitonally [48 (link)].
At specific time points (one week following treatment with chlorambucil, Fludarabine/cyclophosphamide or Rituximab and the next day following treatment with Ibrutinib) animals were sacrificed and single cell solutions produced from their homogenized spleens. CLL cells were sorted by flow-cytometry as demonstrated in the Supplementary Figure 1.

Davies N.J., Kwok M., Gould C., Oldreive C.E., Mao J., Parry H., Smith E., Agathanggelou A., Pratt G., Taylor A.M., Moss P., Griffiths M, & Stankovic T. (2017). Dynamic changes in clonal cytogenetic architecture during progression of chronic lymphocytic leukemia in patients and patient-derived murine xenografts. Oncotarget, 8(27), 44749-44760.

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Pharmacological Inhibition of NLRP3 and BTK

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To pharmacologically inhibit NLRP3 inflammasome, a specific inhibitor MCC950 (Sigma-Aldrich, St. Louis, MO) was injected (IP: 50 mg/Kg) as reported in [42 (link)], starting 72 h before the induction of stress in mice, and again given at every 24 h until the end of the experiment. Control mice were similarly injected with vehicle (0.05% DMSO in saline, i.p.).
To pharmacologically inhibit BTK, a specific inhibitor ibrutinib (PCI-32765, Abcam, Cambridge, MA) was administered (IP: 3 mg/Kg) starting 72 h before the induction of stress in mice, and again given at every 24 h until the end of the experiment. Control mice were injected in parallel with the vehicle (0.05% DMSO in saline, i.p.) at the same time points. To validate the observation from ibrutinib studies, a separate group of mice was injected (IP: 50 mg/kg) with another BTK-specific inhibitor LFM-A13 (Sigma-Aldrich) at similar time points as mentioned above. Control mice were similarly injected with vehicle (0.05% DMSO in saline, i.p.).
To determine the potential therapeutic efficacy of ibrutinib in post-stress paradigm, mice were injected daily with ibrutinib (IP: 3 mg/kg) 2 days after induction of stress in mice. Control mice were injected in parallel with the vehicle (0.05% DMSO in saline, i.p.) at the same time points. ibrutinib and vehicle were administered daily for 5 days.

Ghosh S., Mohammed Z, & Singh I. (2021). Bruton’s tyrosine kinase drives neuroinflammation and anxiogenic behavior in mouse models of stress. Journal of Neuroinflammation, 18, 289.

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CLL Cell-Monocyte Interaction Assay

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CLL cells from patients were stained with Vybrant CFDA SE Cell Tracer (Life Technologies), bound with Alexa-Fluor 594 (Life Technologies) labeled ofatumumab, co-incubated with THP1 cells (ATCC, Manassas, VA) and then assessed for Cell Tracer and Alexa-Fluor 594 staining as previously described (29 , 30 ). THP1 cells were incubated in RPMI1640 media (Life Technologies) containing various concentrations of ibrutinib (Selleckchem, Houston, TX) or vehicle for 1 hour before co-incubation with CLL cells. To abrogate the effect of ibrutinib, THP1 cells were pre-treated overnight with 1μM phorbol 12-myristate 13-acetate (PMA; Sigma, St. Louis, MO) or vehicle (DMSO; Sigma).

Skarzynski M., Niemann C.U., Lee Y.S., Martyr S., Maric I., Salem D., Stetler-Stevenson M., Marti G.E., Calvo K.R., Yuan C., Valdez J., Soto S., Farooqui M.Z., Herman S.E, & Wiestner A. (2015). Interactions between ibrutinib and anti-CD20 antibodies; competing effects on the outcome of combination therapy. Clinical cancer research : an official journal of the American Association for Cancer Research, 22(1), 86-95.

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HBV Mouse Model with Ibrutinib Treatment

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Eight-week old wild-type C57BL/6 mice were purchased from GemPharmatech (Nanjing, China). All mouse experiments were approved by the ethics committee of Quanzhou First Hospital Affiliated to Fujian Medical University. Mice were injected with 5×10¹⁰ viral genome AAV/HBV in 200 µL phosphate-buffered saline in the tail vein. Some mice were treated with 10 mg/kg ibrutinib (CAS: 936563-96-1; Sigma, St. Louis, MO, USA) for 24 h before infection. 14 days post-infection, samples were harvested for analysis.

Lin M., Guo R., Zeng D., Liu J., Zheng M, & Su Z. (2023). IL2-inducible T-cell Kinase is Required for HBV-induced Type T Interferon Expression and Antiviral Response. Journal of Clinical and Translational Hepatology, 11(4), 918-924.

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Btk Inhibitor Ibrutinib Modulates sIgM B Cells

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sIgM^−/− mice were treated with the Btk inhibitor Ibrutinib (PCI-32765; 25 mg/kg/day/mouse; n = 4) diluted in drinking water containing 5% D-Mannitol (Sigma) and 0.5% gelatin (Sigma) or vehicle only (n = 4) for 2 weeks by oral gavage. Control sIgM^+/+ mice (n = 4) were treated with the vehicle only. In two independent experiments sIgM^+/+ mice (n = 5) were treated for 2 or 3 weeks with the vehicle or Ibrutinib (n = 4–5) as above. All mice were fasted for 2 hours before every administration. At the end of the treatment mice were sacrificed and flow cytometric analysis of splenic B cell subsets was performed.

Tsiantoulas D., Kiss M., Bartolini-Gritti B., Bergthaler A., Mallat Z., Jumaa H, & Binder C.J. (2017). Secreted IgM deficiency leads to increased BCR signaling that results in abnormal splenic B cell development. Scientific Reports, 7, 3540.

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Orelabrutinib and Ibrutinib Signaling Pathways

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Orelabrutinib was a gift from INNOCARE (Beijing, China), and ibrutinib was purchased from MedChemExpress (Monmouth Junction, NJ, USA). Orelabrutinib and ibrutinib were dissolved in dimethyl sulfoxide (DMSO) (Sigma Chemical) and stored at −80°C at a suitable stock concentration. Rituximab was preserved in 4°C conditions after being diluted within 24 h. Antibodies against phospho-Tyr42-I kappaB alpha (catalog no. AF7276) and I kappaB alpha (catalog no. AF7776) were purchased from Affinity Biosciences. Antibodies against phospho-Tyr223-BTK, BTK (no. 8547), ITK (no. 2380), phospho-Tyr759-PLCγ2 (no. 3874), PLCγ2 (no. 3872), phospho-Tyr1068-EGF Receptor (D7A5) XP rabbit monoclonal antibody (mAb) (no. 3777), EGF receptor (no. 2232), phospho-Ser536-NF-κB (no. 3039), and NF-κB (no. 8242) were obtained from Cell Signaling Technology (Danvers, MA, USA). Purified mouse anti-BTK (pY551)/ITK (pY511) (cat no. 558034) was provided by BD Biosciences, and anti-β-actin (cat no. A5441) was obtained from Sigma (St. Louis, MO, USA). Anti-APC-CD56 (cat no. 362503) and anti-FITC-CD107a (cat no. 328605) used in flow cytometry were obtained from BioLegend. Anti-EFLUOR450-CD336 (NKp44) (cat no. 48336941) was from Thermo/eBioscience.

Yu H., Wang X., Li J., Ye Y., Wang D., Fang W., Mi L., Ding N., Wang X., Song Y, & Zhu J. (2021). Addition of BTK inhibitor orelabrutinib to rituximab improved anti-tumor effects in B cell lymphoma. Molecular Therapy Oncolytics, 21, 158-170.

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Quantitative Analysis of Drug Transporters

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Dasatinib (DAS), apigenin (APG), and ibrutinib (IBR), were obtained from Sigma-Aldrich (St. Louis, MI, USA). Acetonitrile, formic acid, methanol, and ammonium acetate were purchased from BDH, Pool (UK) and antibodies anti-P-gp/MDR1/ABCB1, anti-BCRP/ABCG2, Anti-CYP3 A2, and anti-β-actin antibodies were obtained from Santacruz (USA).

Raish M., Ahmad A., Shahid M., Jardan Y.A., Ahad A., Kalam M.A., Ansari M.A., Iqbal M., Ali N., Alkharfy K.M, & Al-Jenoobi F.I. (2023). Effects of Apigenin on Pharmacokinetics of Dasatinib and Probable Interaction Mechanism. Molecules, 28(4), 1602.

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Evaluating Ibrutinib's Impact on Melanoma Cells

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The effect of Ibrutinib (Cayman Chemical, Ann Arbor, MI, USA) on the melanoma cell lines was evaluated by the MTT assay. Briefly, 7 × 10³ cells were seeded in 96-well plates. After 24 h, they were treated with different concentrations of Ibrutinib (1, 2, 2.5, 3, 5, 10, 25, 50 and 100 μmol/L) for 48 h. Following, 10 μL of MTT reagent (5 mg/mL; Sigma-Aldrich, St. Louis, MO, USA) was added to each well and the plates were incubated for 4 h protected from light. After this period, the MTT solution was removed, replaced by 100 μL of dimethylsulfoxide (DMSO), and the plate was homogenized for 15 min to dissolve the formed formazan crystals. Absorbance was measured in the spectrophotometer Synergy H1 (Agilent BioTek, Santa Clara, CA, USA) at 570 nm. Then, the IC₅₀ dose of Ibrutinib was determined.

Lins F.V., Bispo E.C., Rodrigues N.S., Silva M.V., Carvalho J.L., Gelfuso G.M, & Saldanha-Araujo F. (2024). Ibrutinib Modulates Proliferation, Migration, Mitochondrial Homeostasis, and Apoptosis in Melanoma Cells. Biomedicines, 12(5), 1012.

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Ibrutinib and Perindopril in Rat Model

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All animal procedures in this study were conducted in accordance with the Health Guide for the Care and Use of Laboratory Animals and approved by the Animal Care Committee at Harbin Medical University (IACUC number: 2021121) to ensure humane care. Seventy male SD rats weighing 260-280g with a mean age of 8 weeks were obtained from Beijing Vital River Laboratory Animal Technology Co, Ltd (Beijing, China) and housed at the Experimental Animal Center of Harbin Medical University. The rats were randomly assigned and individually housed in a 12:12 h light-dark cycle, with ad libitum access to food and water. For the experimental groups, rats in the ibrutinib group were orally administered ibrutinib (17 mg/kg/d; Catalent CTS, LLC, USA) for a duration of 4 weeks. The dosage of ibrutinib was determined based on body surface area, as previously described.¹⁰ (link) Rats in the ibrutinib + perindopril group received both ibrutinib and perindopril (2 mg/kg/d³⁴ (link)) orally for 4 weeks. Control rats received the vehicle solution in parallel. The vehicle solution was prepared using dimethylsulfoxide (DMSO; Sigma-Aldrich, Natick, MA, USA) as a solvent for dissolving ibrutinib.

Yan S., Xu W., Fang N., Li L., Yang N., Zhao X., Hao H., Zhang Y., Liang Q., Wang Z., Duan Y., Zhang S., Gong Y, & Li Y. (2024). Ibrutinib-induced pulmonary angiotensin-converting enzyme activation promotes atrial fibrillation in rats. iScience, 27(2), 108926.

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Pancreatic Cancer Cell Line Culture

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The human pancreatic cancer cell lines PANC-1 and Capan2 were purchased from the Stem Cell Bank of Type Culture Collection of the Chinese Academy of Sciences (Shanghai, China). PANC-1 and Capan2 cells were cultured in DMEM or RPMI-1640 medium supplemented with 10% FBS in an atmosphere of 5% CO2 at 37 °C. Ibrutinib (PCI-32765, 99.2%) was purchased from Selleck, USA. Ibr-7 (Lot: 20161216, > 95%) was provided by Hangzhou Hezheng Pharmaceutical Co., Ltd. Ibrutinib and Ibr-7 were dissolved in DMSO (Sigma-Aldrich, St Louis, Missouri, USA) at a concentration of 100 mmol/L and stored at − 20 °C.

Tan B., Dong R., Zhang B., Yan Y., Li Q., Wang F, & Lin N. (2020). The Ibr-7 derivative of ibrutinib radiosensitizes pancreatic cancer cells by downregulating p-EGFR. Cancer Cell International, 20, 458.

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