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

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

Cat. No.: HY-50896 Purity: 99.99%
Handling Instructions

Erlotinib is a medication for the treatment of non-small cell lung cancer. It inhibits purified EGFR kinase with an IC50 of 2 nM.

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

Erlotinib Chemical Structure

Erlotinib Chemical Structure

CAS No. : 183321-74-6

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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Erlotinib:

Top Publications Citing Use of Products

    Erlotinib 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 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 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 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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Erlotinib is a medication for the treatment of non-small cell lung cancer. It inhibits purified EGFR kinase with an IC50 of 2 nM.

    IC50 & Target[1]

    EGFR

    2 nM (IC50, Cell Free Assay)

    In Vitro

    Erlotinib (CP-358,774) 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

    Under the experimental conditions, the combination of B-DIM and Erlotinib (50 mg/kg, i.p.) treatment shows significant decrease (P <0.01) in tumor weight compared with untreated control[2]. Erlotinib (20 mg/kg, p.o.) significantly attenuates Cisplatin (CP)-induced body weight (BW) loss when compared to the CP+vehicle (V) rats (P<0.05). Erlotinib treatment significantly improves renal function in CP-N(normal control group, NC) rats. The CP+Erlotinib (E) rats show significant reduction of the levels of Serum creatinine (s-Cr) (P<0.05), blood urea nitrogen (BUN) (P<0.05), urinary N-acetyl-β-D-glucosaminidase (NAG) index (P<0.05), and significant increase of urine volume (UV) (P<0.05) and Cr clearance (Ccr) (P<0.05) compare to the CP+V rats[3]

    Clinical Trial
    Molecular Weight

    393.44

    Formula

    C₂₂H₂₃N₃O₄

    CAS No.

    183321-74-6

    SMILES

    C#CC1=CC=CC(NC2=NC=NC3=C2C=C(C(OCCOC)=C3)OCCOC)=C1

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (127.08 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5417 mL 12.7084 mL 25.4168 mL
    5 mM 0.5083 mL 2.5417 mL 5.0834 mL
    10 mM 0.2542 mL 1.2708 mL 2.5417 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2 mg/mL (5.08 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2 mg/mL (5.08 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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
    [2][3]

    Mice[2]
    Female ICR-SCID (6-7 weeks old) mice are randomized into the following treatment groups (n=7): (a) untreated control; (b) only B-DIM (50 mg/kg body weight), intragastric once every day; (c) Erlotinib (50 mg/kg body weight), everyday i.p. for 15 days; and (d) B-DIM and Erlotinib, following schedule as for individual treatments. All mice are killed on day 3 following last dose of treatment, and their body weight is determined. One part of the tissue is rapidly frozen in liquid nitrogen and stored at −70°C for future use and the other part is fixed in formalin and processed for paraffin block. H&E staining of fixed tissue section is used to confirm the presence of tumor(s) in each pancreas.
    Rats[3]
    Six-week-old male Sprague-Dawley (SD) rats weighing 180 to 210 g are used. Cisplatin (CP) is freshly prepared in saline at a concentration of 1 mg/mL and then injected intraperitoneally in SD rats (n=28) at a dose of 7 mg/kg on day 0. To investigate the effect of Erlotinib, 28 CP-N rats are divided into two groups. Separate groups (n=14) each of animals are administered with either Erlotinib (20 mg/kg) (CP+E, n=14) or vehicle (CP+V, n=14) daily by oral gavage from day -1 (24 hours prior to the CP injection) to day 3. Vehicle-treated groups receive an equivalent volume of saline. Five male SD rats at the age of 6 weeks are used as a normal control group (NC, n=5). The NC rats are given an equivalent volume of saline daily by oral gavage from day -1 to day 3. At day 4 (96 hours after CP injection), each rat is anesthetized and sacrificed by exsanguination after the cardiac puncture; blood is collected by cardiac puncture and kidneys are collected. Renal tissue is divided; separate portions are snap-frozen in liquid nitrogen or fixed in 2% paraformaldehyde/phosphate-buffered saline (PBS) for later use. All surgery is performed under diethyl ether gas anesthesia, and all efforts are made to minimize suffering.

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

    References
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