EGF (Peprotech) was used at 100 ng/mL, and Nrg was used at 10 ng/mL. Drug pretreatment was as follows: 50 µM EIPA (Sigma-Aldrich) for 60 min, 25 µM HCQ (Sigma-Aldrich) for 48 h, 2.5 µM FTY720 (Cayman) for 48 h, 1 µM GDC0941 (Selleck) for 1 h, 40 µM ketoconazole (Sigma-Aldrich) for 72 h (sensitivity) or 24 h (recycling), 1 µM BIBW2992 (Selleck) for 1 h, 10 mM MβCD (Sigma-Aldrich) for 30 min, 10 µM latrunculin A (Cayman) for15 min, 5 µM jasplakinolide for 15 min, and 50 µg/mL cyclohexamide (Sigma-Aldrich) for 1 h. These doses were maintained throughout the experiment.
Bibw2992
Manufactured by Selleck Chemicals
Sourced in United States
BIBW2992 is a chemical compound used in research laboratory settings. It functions as a tyrosine kinase inhibitor, specifically targeting the epidermal growth factor receptor (EGFR). This product is intended for use in scientific research applications.
Automatically generated - may contain errors
Lab products found in correlation
Afatinib, by Selleck Chemicals (2 mentions)
Ketoconazole, by Merck Group (1 mentions)
Gdc 0941, by Selleck Chemicals (1 mentions)
Jasplakinolide, by Merck Group (1 mentions)
Cyclohexamide, by Merck Group (1 mentions)
Latrunculin a, by Cayman Chemical (1 mentions)
Epidermal growth factor (egf), by Thermo Fisher Scientific (1 mentions)
Fty720, by Cayman Chemical (1 mentions)
Phenformin, by Merck Group (1 mentions)
Aicar, by Cell Signaling Technology (1 mentions)
Azd8055, by Selleck Chemicals (1 mentions)
Rapamycin, by LC Laboratories (1 mentions)
Metformin, by Merck Group (1 mentions)
Erlotinib, by LC Laboratories (1 mentions)
Afatinib, by Thermo Fisher Scientific (1 mentions)
Crizotinib pf 02341066, by Selleck Chemicals (1 mentions)
Bio plex manager software version 4, by Bio-Rad (1 mentions)
Bio plex 200 system, by Bio-Rad (1 mentions)
Dasatinib, by Selleck Chemicals (1 mentions)
Etoposide, by Selleck Chemicals (1 mentions)
6 protocols using bibw2992
1
Investigating Receptor Signaling Modulation
2
Pharmacological Compounds for Cell Signaling
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3
Multiplex Cytokine Profiling of Choriocarcinoma
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Using a Luminex® xMAP® platform in a magnetic bead format, we simultaneously studied the following analytes from the culture supernatants of MUG-Chor1 and UM-Chor1 cells: epidermal growth factor (EGF), tumour necrosis factor alpha (TNFα), vascular endothelial growth factor (VEGF), and fibroblast growth factor 2 (FGF2). No cross-reactivity was noted between the antibodies for an analyte or between any of the other analytes in this panel. Treatment was performed with 4 μM crizotinib (PF-02341066; SelleckChem, Houston, TX, USA), 0.16 μM afatinib (BIBW2992; SelleckChem), or with a simultaneous co-dosing of crizotinib and afatinib for 72 h. For detection, we used a commercially available Procarta Plex (Thermo Fisher, Waltham, MA, USA) on a Bioplex200 system (Bio-Rad Laboratories, Hercules, CA, USA) according to the manufacturers´ instructions. Measurement of mean fluorescence intensities was performed using Bio-Plex Manager software, version 4.1 (Bio-Rad Laboratories, Hercules, CA, USA) with a 5-parametric curve fitting.
4
Investigating Signaling Pathways in Cancer
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Dasatinib, BIBW2992, PD0325091 and Etoposide were purchased from Selleck Chemicals (Houston, TX) and prepared as 20 mM stock solutions in DMSO. Antibodies used included anti-YAP-TAZ, pLats, Lats1, Lats2, pMST1/2, pH2AX, MEK, pMEK(S217/221), ERK, pERK(T202/Y204), pRb, pS6, LC3A/B, ATM, pChk1, Chk1, pChk2, Chk2, pCDC25c, pATRIP, p27, p21, pp38, β-catenin, cyclin D1, survivin, p4EBP1, pSMAD2(S465–467), p70S6K, pCDC2, CDC6, γH2AX, ATR, pDNA-PK(S2056) and DNA-PK, (Cell Signaling Technology, Danvers, MA); BRAF and cyclin E (Santa Cruz, Dallas, TX) and ATM, Flag M2 and β-actin (Sigma-Aldrich, St. Louis, MO); pATM(S1981) (GeneTex, Irvine, CA). Predesigned siRNAs of the target genes were purchased from Dharmacon (Pittsburgh, PA) or Thermo Scientific (Rodckford, IL). pcDNA4-Chk1-Flag and pCMV5-TOPO-3Xflag-TAZ plasmids were purchased from Addgene (Cambridge, MA). WTBRAF plasmid was provided by Dr. W. Kolch (Systems Biology Irland and The Conway Institute, University College Dublin).
5
EGFR Inhibitor Evaluation in Keratinocytes
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Cells were grown on either glass coverslips, dishes or plates prior to DMSO and drug treatments. The MEK inhibitor U0126 (#V1121, Promega Corporation, WI, USA) and the EGFR inhibitors AG1478 (#658552, Calbiochem, MA, USA), lapatinib (#11493, Cayman Chemical, MI, USA), erlotinib (#S7786; Selleckchem, TX, USA), gefitinib (ZD1839; #S1025; Selleckchem, TX, USA) and afatinib (BIBW2992; #S1011; Selleckchem, TX, USA) were all dissolved in DMSO. The structures of afatinib (CHEMBL1173655), erlotinib (CHEMBL553), gefitinib (CHEMBL939) and lapatinib (CHEMBL554) were retrieved from ChEMBL database (https://www.ebi.ac.uk/chembl/ ). For the EGF study, NEB-1 mutant cells were cultured in medium without EGF (EGF−) for two passages (∼14 days) before the experiments involving serum starvation, EGF re-stimulation for 3 h with or without AG1478 (10 µM) for 1 h. Alternatively, N/TERT-1 wild-type or mutant cells were re-stimulated with EGF for 6 h after afatinib washout.
6
Compound Screening for Cancer Therapeutics
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EGF, basic fibroblast growth factor (bFGF), and Wnt3a were purchased from R&D Systems (Minneapolis, MN). AG1478 (a reversible EGFR-TKI) was purchased from Wako (Tokyo, Japan). BIBW2992 (an irreversible EGFR-TKI) and TAE684 (an ALK inhibitor) were purchased from Selleck Chemicals (Houston, TX). XAV939 (a β-Catenin inhibitor) and cisplatin (cis-diamminedichloroplatinum [CDDP]) were purchased from Sigma-Aldrich. For the in vitro studies, stock solutions were prepared in dimethyl sulfoxide. For the in vivo studies, BIBW2992 was suspended in a vehicle (0.5% methylcellulose [w/v] in sterile water) for oral administration to mice bearing xenograft tumors.
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