1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Autophagy
  2. EGFR
    Autophagy
  3. Erlotinib mesylate

Erlotinib mesylate (Synonyms: CP-358774 mesylate; NSC 718781 mesylate; OSI-774 mesylate)

Cat. No.: HY-12008A
Handling Instructions

Erlotinib mesylate (CP-358774 mesylate) inhibits purified EGFR kinase with an IC50 of 2 nM.

For research use only. We do not sell to patients.

Erlotinib mesylate Chemical Structure

Erlotinib mesylate Chemical Structure

CAS No. : 248594-19-6

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Top Publications Citing Use of Products

    Erlotinib mesylate purchased from MCE. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321.

    Western blot analysis of total and phosphorylated EGFR expression in two breast cancer cells pretreated with different concentration Erlotinib for 4h.

    Erlotinib mesylate purchased from MCE. Usage Cited in: Oncogene. 2017 May 11;36(19):2643-2654.

    Effects of anti-cancer agents Oxaliplatin (25 mM), Erlotinib (25 mM) and cAMP inducer Forskolin (25 mM) on FOXO3 expression in Panc-1 cells are assessed for 72h (n=3).

    Erlotinib mesylate purchased from MCE. Usage Cited in: Anal Chim Acta. 2018 Nov 22;1032:138-146.

    30 min after EGF(100 ng/mL) and EGFP-sSH2(Arg)9 (5 μM) are added into the MDA-MB-468 cell culture medium, Erlotinib is added into the cell culture medium (100 nM), and the picture was collected at 30 min after Erlotinib treatment.

    Erlotinib mesylate purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 21;9:660.

    By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (erlotinib), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.

    Erlotinib mesylate purchased from MCE. Usage Cited in: Cancer Med. 2019 Nov 5. 

    Western blots of proteins expression in EGFR signaling pathways in LN229 and U87 cells with MYST1/GFP overexpression after erlotinib (200 ng/mL)/DMSO treatment.
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    Description

    Erlotinib mesylate (CP-358774 mesylate) inhibits purified EGFR kinase with an IC50 of 2 nM.

    IC50 & Target[1]

    EGFR

    2 nM (IC50)

    In Vitro

    Erlotinib mesylate (CP-358774 mesylate) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC50 of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC50 of 100 nM for an 8-day proliferation assay[1]. The combination of B-DIM and Erlotinib (2 μM) results in a significant inhibition of colony formation in BxPC-3 cells when compared with either agent alone. The combination of B-DIM and Erlotinib (2 μM) results in a significant induction of apoptosis only in BxPC-3 cells when compare with the apoptotic effect of either agent alone[2].

    In Vivo

    There is a 1.49-fold statistically significant difference between AUC0-inf after p.o. administration of Erlotinib (5 mg/kg) comparing Bcrp1/Mdr1a/1b-/- and WT mice (7,419±1,720 versus 4,957±1,735 ng*h/mL respectively, P=0.01)[3]. The administration of Erlotinib (10 mg/kg/day, or 20 mg/kg/day) to Bleomycin (BLM)-treated rats shows no exacerbation of lung injuries in indices such as macroscopic findings, lung weights, histopathological scores (lung lesion density and lung fibrosis score), and pulmonary hydroxyproline (HyP) level. The result suggests that Erlotinib does not have any exacerbating effects on lung injuries induced by BLM in rats[4].

    Clinical Trial
    Molecular Weight

    489.54

    Formula

    C₂₃H₂₇N₃O₇S

    CAS No.

    248594-19-6

    SMILES

    CS(=O)(O)=O.COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    Kinase Assay
    [1]

    The kinase reaction is performed in 50 μL of 50 mM HEPES (pH 7.3), containing 125 mM NaCl, 24 mM MgCl2, 0.1 mM Na3VO4, 20 μM ATP, 1.6 μg/mL EGF, and 15 ng of EGFR, affinity purified from A431 cell membranes. The compound in DMSO is added to give a final DMSO concentration of 2.5%. Phosphorylation is initiated by addition of ATP and proceeded for 8 mm at room temperature, with constant shaking. The kinase reaction is terminated by aspiration of the reaction mixture and is washed 4 times with wash buffer. Phosphorylated PGT is measured by 25 mim of incubation with 50 μL per well HRP-conjugated PY54 antiphosphotyrosine antibody, diluted to 0.2 μg/mL in blocking buffer (3% BSA and 0.05% Tween 20 in PBS). Antibody is removed by aspiration, and the plate is washed 4 times with wash buffer. The colonmetric signal is developed by addition of TMB Microwell Peroxidase Substrate, 50 μL per well, and stopped by the addition of 0.09 M sulfuric acid, 50μL per well. Phosphotyrosine is estimated by measurement of absorbance at 450 nm. The signal for controls is typically 0.6-1.2 absorbance units, with essentially no back ground in wells without AlP, EGFR, or POT and is proportional to the time of incubation for 10 mm[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    To test the viability of cells treated with B-DIM, Erlotinib, or the combination, BxPC-3 and MIAPaCa cells are plated (3,000-5,000 per well) in a 96-well plate and incubated overnight at 37°C. A range of concentrations for both B-DIM (10-50 µM) and Erlotinib (1-5 µM) is initially tested. Based on the initial results, the concentration of B-DIM (20 µM) and Erlotinib (2 µM) are chosen for all assays. The effects of B-DIM (20 µM), Erlotinib (2 µM), and the combination on BxPC-3 and MIAPaCa cells are determined by the standard MTT assay after 72 h and is repeated three times. The color intensity is measured by a Tecan microplate fluorometer at 595 nm. DMSO-treated cells are considered to be the untreated control and assigned a value of 100%. In addition to the above assay, we have also done clonogenic assay for assessing the effects of treatment[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    Mice[3]
    Bcrp1/Mdr1a/1b-/- and WT mice are treated p.o. or i.p. with 5 mg/kg Erlotinib. The i.p. administration is chosen assuming good drug absorption and complete bioavailability. Sampling is done from the tip of the lateral tail vein in three series. During the first series, whole blood samples are collected at 15 min and 0.5, 1.5, 5, and 10 h after injection. Based on the results of this initial group, the sampling times of the two subsequent series are adapted to 5 and 15 min and 0.5, 1.5, 4, and 8 h after injection. After collection, the blood samples are immediately centrifuged and plasma is stored at -20°C until high-performance liquid chromatographic analysis took place.
    Rats[4]
    Seven-week-old male Crl:CD (SD) rats (244-297 g) are used. The animals are treated with Erlotinib (10 mg/kg and 20 mg/kg) orally by gavage.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Keywords:

    ErlotinibCP-358774NSC 718781OSI-774CP358774CP 358774NSC718781NSC-718781OSI774OSI 774EGFRAutophagyEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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