Erlotinib hcl

Manufactured by Selleck Chemicals

Sourced in United States

Erlotinib HCl is a chemical compound used in research and laboratory settings. It is a tyrosine kinase inhibitor that can be used to study cellular signaling pathways.

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Lab products found in correlation

Osimertinib, by Selleck Chemicals (1 mentions) Carboplatin, by Selleck Chemicals (1 mentions) Hydroxypropyl methylcellulose, by Merck Group (1 mentions) Paclitaxel, by Selleck Chemicals (1 mentions) Cisplatin, by Selleck Chemicals (1 mentions) 6 thio dg, by Merck Group (1 mentions) Gemcitabine hcl, by Selleck Chemicals (1 mentions) Pegfr y1068, by Cell Signaling Technology (1 mentions) P s6 ribosomal protein, by Cell Signaling Technology (1 mentions) α tubulin, by Merck Group (1 mentions) P erk1 2, by Cell Signaling Technology (1 mentions) P akt ser473, by Cell Signaling Technology (1 mentions) S6 ribosomal protein, by Cell Signaling Technology (1 mentions) Erk1 2, by Cell Signaling Technology (1 mentions) Afatinib, by LC Laboratories (1 mentions) Gsk1838705a, by Selleck Chemicals (1 mentions) Recombinant human egf, by Thermo Fisher Scientific (1 mentions) Hepg2, by American Type Culture Collection (1 mentions) Hep3b, by American Type Culture Collection (1 mentions) Sorafenib, by Bayer (1 mentions)

Spelling variants of this product

Erlotinib (299 citations) Erlotinib HCl (OSI-744) (5 citations)

11 protocols using erlotinib hcl

Regulation of Pancreatic Cancer Cells by Reg3g and DCs

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Panc02 cells were incubated with:

media alone (control); conditioned media from DCs of TBM (DC); conditioned media from DCs of Reg3g-treated TBM (DC-Reg3g); conditioned media from DCs of TBM in combination with 100 ng/ml Reg3g (Reg3g+DC); and 100 ng/ml Reg3g alone for 24 h to determine cell viability, secretion of IL-10, and TGF-β, migration and invasion assessed by crystal violet staining.^{7 (link)} All experiments were performed in duplicate for each sample.

media alone (control); incubated with 50 μM Erlotinib HCL (EGFR-specific inhibitor; Selleck, Houston, TX, USA) for 24 h (Erlotinib); incubated with 100 ng/ml Reg3g for 24 h (Reg3g); incubated with 50 μM Erlotinib HCL and 100 ng/ml Reg3g for 24 h (Erlotinib+Reg3g).

DCs from TBM were exposed to:

PBS; 100 ng/ml Reg3g, respectively.

media alone (control); incubated with 50 μM Erlotinib HCL (EGFR-specific inhibitor; Selleck) for 24 h (Erlotinib); incubated with 100 ng/ml Reg3g for 24 h (Reg3g); incubated with 50 μM Erlotinib HCL and 100 ng/ml Reg3g for 24 h (Erlotinib+Reg3g).

DCs from control mice were exposed to: TME, 10% Panc02-conditioned medium; and Reg3g+TME, respectively. DCs were treated with 10 μM AG490 (Sigma) for 6 days to suppress the expression of STAT3.

Liu X., Zhou Z., Cheng Q., Wang H., Cao H., Xu Q., Tuo Y., Jiang L., Zou Y., Ren H, & Xiang M. (2017). Acceleration of pancreatic tumorigenesis under immunosuppressive microenvironment induced by Reg3g overexpression. Cell Death & Disease, 8(9), e3033-.

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Preparation and Formulation of Anticancer Agents

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For in vitro studies, 6-thio-dG (Metkinen Oy, Kuopio, Finland) was dissolved in DMSO/water (1:1) to prepare 10 mM stock solutions, which were kept frozen at −20°C. A 1 mM, final concentration stock was prepared for in vitro experiments and added in fresh medium at different concentrations. Erlotinib HCl (Selleckchem, Houston, TX) was dissolved in DMSO to prepare 10 mM stock solutions, which were kept frozen at −80°C. A 2.5 μM erlotinib final concentration was used for in vitro experiments. Osimertinib and paclitaxel (Selleckchem) were dissolved in DMSO, and carboplatin (Selleckchem) was dissolved in water to prepare 10 mM stock solutions, which were kept frozen at −80°C. A 1 mM final concentration stock was prepared for in vitro experiments and added in fresh medium at different concentrations.
For mouse in vivo studies, 6-thio-dG was prepared in 5% DMSO for intraperitoneal (i.p.) injection or 0.4% (hydroxypropyl)methyl cellulose (Sigma, Saint Louis, MO) for oral gavage. Erlotinib was prepared in 15% Captisol (β-cyclodextrin, sulfobutyl ethers, sodium salts) (Cydex Pharmaceuticals, Lawrence, KS) for oral gavage. Gemcitabine HCl and cisplatin (Selleckchem) were dissolved in 0.9% NaCl saline solution for i.p. injections.

Mender I., LaRanger R., Luitel K., Peyton M., Girard L., Lai T.P., Batten K., Cornelius C., Dalvi M.P., Ramirez M., Du W., Wu L.F., Altschuler S.J., Brekken R., Martinez E.D., Minna J.D., Wright W.E, & Shay J.W. (2018). Telomerase-Mediated Strategy for Overcoming Non–Small Cell Lung Cancer Targeted Therapy and Chemotherapy Resistance. Neoplasia (New York, N.Y.), 20(8), 826-837.

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Erlotinib and Afatinib Inhibitor Assay

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Erlotinib HCl (Selleckchem, TX, USA) was dissolved in dimethyl sulfoxide (DMSO; Sigma) at a stock concentration of 10 mM and diluted in culture medium for use. Afatinib (LC Laboratories, Woburn, MA, USA) was dissolved in DMSO at a stock concentration of 40 mM, and further diluted in culture medium to the required concentrations. Primary antibodies used in these studies were EGFR (#2232), pEGFR^Y1068 (#2234), AKT (#2938), pAKT^ser473 (#4060), ERK1/2 (#9102), pERK1/2 (#9101), S6 ribosomal protein (#2317), pS6 ribosomal protein (#2211; Cell Signaling Technology), periplakin (clone EPR8296; ab131269; Abcam) and α-tubulin (T5158; Sigma). The secondary antibodies goat anti-rabbit IgG-HRP (SB4010-05) and goat anti-mouse IgG-HRP (SB1010-05) were purchased from Southern Biotech. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT; Sigma-Aldrich) solution was prepared at 5 mg/ml in phosphate-buffered saline (PBS).

Lee H.M., Kelly G.M., Zainal N.S., Yee P.S., Fadlullah M.Z., Lee B.K., Gan C.P., Patel V, & Cheong S.C. (2019). The 4717C > G polymorphism in periplakin modulates sensitivity to EGFR inhibitors. Scientific Reports, 9, 2357.

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Anticancer Compound Screening in Human HCC Cells

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Regorafenib and Sorafenib were gifts from the Bayer Corp (West Haven, CT,USA). Recombinant human EGF was purchased from Pepro-Tech (Rocky Hill, NJ, USA). Erlotinib HCl and GSK1838705A were purchased from Selleckchem (Houston, TX, USA). Hep3B, HepG2, and PLC/PRF/5 human HCC cells were purchased from the American Type Culture Collection (ATCC, Rockville, MD, USA). The culture medium was Dulbecco's modified eagle's medium (DMEM). All cell culture components were purchased from Sigma-Aldrich (Milan, Italy).

D'Alessandro R., Refolo M.G., Lippolis C., Carella N., Messa C., Cavallini A, & Carr B.I. (2015). Modulation of Regorafenib effects on HCC cell lines by epidermal growth factor. Cancer chemotherapy and pharmacology, 75(6), 1237-1245.

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Antibody Validation for Cell Signaling Studies

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Rabbit monoclonal antibodies against HSP27, HSP90, FEN1, phosphor-H2AX (Ser139), EGFR, phospho-EGFR (Y1068), Akt, phospho-Akt (Ser473) and mouse monoclonal antibody against ubiquitin (Ub) were purchased from Cell Signaling Technology (Beverly, MA, USA). Mouse monoclonal antibody against HSP70 was obtained from Stressgen Bioreagents (Victoria, BC, Canada). Pol β polyclonal antibody was obtained from Abcam (Cambridge, United Kingdom). Rabbit polyclonal antibodies against GAPDH and Flag-tag were obtained from Bioworld Biotechnology (Minneapolis, MN, USA). Rabbit polyclonal antibody against HA-tag was obtained from Santa Cruz Biotechnology (Wembley, Middlesex, UK). Secondary antibodies coupled to IRDye800 fluorophore were purchased from Rockland (Gilbertsville, PA, USA). Erlotinib HCL (CAS: 183319-69-9) and Gefitinib (CAS: 184475-35-2) were from Selleckchem (Houston, TX, USA). Methyl methanesulfonate (MMS), MG132, NH₄Cl, 6-Thioguanine (6-TG) and adenosine triphosphate (ATP) were obtained from Sigma-Aldrich (St. Louis, MO, USA). Cycloheximide (CHX) was obtained from Calbiochem (San Diego, Calif., USA). Hydrogen peroxide (H₂O₂) was obtained from Merck (Darmstadt, Germany).

Cao X., Zhou Y., Sun H., Xu M., Bi X., Zhao Z., Shen B., Wan F., Hong Z., Lan L., Luo L., Guo Z, & Yin Z. (2018). EGFR-TKI-induced HSP70 degradation and BER suppression facilitate the occurrence of the EGFR T790M resistant mutation in lung cancer cells. Cancer letters, 424, 84-96.

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EGFR-expressing Human Prostate Cancer Cell Lines

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The EGFR-expressing human PCa cell lines LNCaP, DU145, ad PC-3 were obtained from the American Type Culture Collection (ATCC, Manassas, VA, USA). Cell line identity was verified by short tandem repeat (STR) analysis (CLS GmbH, Eppelheim, Germany). A Chinese hamster ovary (CHO) cell line with lack of human EGFR expression served as EGFR-negative control and was purchased from Gibco (Gibco, Invitrogen, Karlsruhe, Germany). LNCaP, DU145 and PC-3 cells were routinely propagated in complete RPMI 1640 medium, and CHO cells were propagated in complete F-12 medium (Gibco, Invitrogen, Karlsruhe, Germany), each with 10% fetal bovine serum (Biochrom, Berlin, Germany), penicillin (100 U/mL) and streptomycin (100 mg/L) as supplements, and incubated at 37 °C and 5% CO₂ to maintain exponential cell growth and proliferation. Erlotinib HCl (Selleck Chemicals Llc, Houston, TX, USA) was dissolved in DMSO as a 4 mg/mL stock solution, aliquoted and stored at −80 °C until use.

Fischer A., Wolf I., Fuchs H., Masilamani A.P, & Wolf P. (2020). Pseudomonas Exotoxin A Based Toxins Targeting Epidermal Growth Factor Receptor for the Treatment of Prostate Cancer. Toxins, 12(12), 753.

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Chemical Library Screening for Novel Therapeutics

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The SelleckChem library from the Molecular Screening Facility at the Wistar Institute was used for initial screens. However, once hits were identified, additional material was purchased for further testing. Mubritinib (S2216), Carmofur (S1289), Erlotinib HCl (S1023), NSC-207895 (S2678), OSI-420 (S2205), Emodin (S2295), TAK-285 (S2784), and Deguelin (S8132) were purchased from SelleckChem. Linifanib (M15676), Regorafenib (R16040), and Afatinib (G-7208) were purchased from AChemBlock. Adrucil (228440010) and Cytarabine (449561000) were purchased from Acros Organics. Lenalidomide (6305/100) and Dopamine HCl (3548/50) were purchased from Tocris Bioscience. Dacomitinib (PZ0330) and Rotenone (R8875) were purchased from Sigma. Rapamycin (J62473) was purchased from Alfa Aesar.

Calderon A., Soldan S.S., De Leo A., Deng Z., Frase D.M., Anderson E.M., Zhang Y., Vladimirova O., Lu F., Leung J.C., Murphy M.E, & Lieberman P.M. (2020). Identification of Mubritinib (TAK 165) as an inhibitor of KSHV driven primary effusion lymphoma via disruption of mitochondrial OXPHOS metabolism. Oncotarget, 11(46), 4224-4242.

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Cell culture media for erlotinib studies

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We made use of two types of media in our experiments. First, ‘erlotinib-free media' is composed of RPMI 1640 (Corning #10 040 CM) supplemented with 5% fetal bovine serum (Life Technologies #16140-071) and 1% Antibiotic-Antimycotic (Life Technologies #15240-062). Second, ‘erlotinib media' is composed of erlotinib-free media and 2.5 μM erlotinib HCl (Selleckchem, Cat.#S1023). Unless otherwise stated, all experiments with PC9 and PC9-1 were performed in ‘erlotinib-free media' and experiments with PERCs were performed in ‘erlotinib media'.

Ramirez M., Rajaram S., Steininger R.J., Osipchuk D., Roth M.A., Morinishi L.S., Evans L., Ji W., Hsu C.H., Thurley K., Wei S., Zhou A., Koduru P.R., Posner B.A., Wu L.F, & Altschuler S.J. (2016). Diverse drug-resistance mechanisms can emerge from drug-tolerant cancer persister cells. Nature Communications, 7, 10690.

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Erlotinib Inhibits GPCMV Viral Replication

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erlotinib HCl (OSI-744; SelleckChem) solution was prepared at 20 mg/ml (46.52 mM) in DMSO. On day 0, GPL (or REPI) cells were pretreated with 0 nM (untreated control), 10 nM, 50 nM, 500 nM, 1 μM, or 10μM erlotinib (OSI-744; SelleckChem) for 1.5 h at 37°C with 5% CO₂. Cells were then infected separately with either GPCMV(PC+) or GPCMV(PC−) at moi 0.5 pfu/cell for 1 h. Inoculum was washed, and monolayers were overlaid with fresh media containing the same concentration of inhibitor as pretreatment, respectively. After 72 h incubation at 37°C/5% CO₂, supernatants and monolayers were harvested and titrated in duplicate on GPL cells as previously described [30 (link)]. Experiments were carried out in triplicate. Cell viability was assayed by CellTiter-Glo® Luminescent Cell Viability Assay (Promega) following manufacturer’s protocol. Viability assays were carried out on cells in the presence and absence of drugs (at concentrations used in viral assays) as well as control DMSO only in media. During cell viability assays, cells were not infected with virus but incubated in presence of drugs for similar duration as virus studies. Experiments were carried out in triplicate for each assay condition.

El-Hamdi N.S., Choi K.Y, & McGregor A. (2020). Guinea pig cytomegalovirus trimer complex gH/gL/gO uses PDGFRA as universal receptor for cell fusion and entry. Virology, 548, 236-249.

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Cell Line Culturing and Drug Treatment

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Cell lines and reagents. Human urinary BC cell lines T24 (transitional cell carcinoma) and HT-1376 (grade 3, carcinoma) were purchased from the American Type Culture Collection (Manassas, VA, USA) and cultured in Dulbecco's modified Eagle medium (Gibco, Invitrogen, Karlsruhe, Germany) with 10% fetal calf serum (Biochrom, Berlin, Germany) and penicillin/streptomycin (100 U/ml, 100 mg/l) at 37˚C and 5% CO 2 . Verification of the cell lines was performed by short tandem repeat analysis (CLS GmbH, Eppelheim, Germany). CHO cell line was cultured in Ham´s F12 nutrient mix medium (Gibco, Invitrogen) with 10% fetal calf serum (Biochrom) and penicillin/streptomycin (100 U/ml, 100 mg/l) at 37˚C and 5% CO 2 as control. Erlotinib HCl (Selleck Chemicals Llc, Houston, TX, USA) was dissolved as 4 mg/ml stock solution in DMSO and stored at -80˚C until use.

Masilamani A.P., Fischer A., Schultze-Seemann S., Kuckuck I., Wolf I., Dressler F.F., Gratzke C, & Wolf P. (2021). Epidermal Growth Factor Based Targeted Toxin for the Treatment of Bladder Cancer. Anticancer research, 41(8).

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