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

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

Cat. No.: HY-12008 Purity: 99.81%
COA Handling Instructions

Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

Erlotinib Hydrochloride Chemical Structure

Erlotinib Hydrochloride Chemical Structure

CAS No. : 183319-69-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 76 publication(s) in Google Scholar

Other Forms of Erlotinib Hydrochloride:

Top Publications Citing Use of Products

71 Publications Citing Use of MCE Erlotinib Hydrochloride

WB
IF

    Erlotinib Hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Med. 2019 Dec;8(18):7793-7808.  [Abstract]

    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.

    Erlotinib Hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321.  [Abstract]

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

    Erlotinib Hydrochloride purchased from MedChemExpress. Usage Cited in: Anal Chim Acta. 2018 Nov 22;1032:138-146.  [Abstract]

    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 Hydrochloride purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 21;9:660.  [Abstract]

    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 Hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2017 May 11;36(19):2643-2654.  [Abstract]

    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).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    IC50 & Target[1]

    EGFR

    2 nM (IC50)

    In Vitro

    Erlotinib Hydrochloride (CP-358774 Hydrochloride) 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].

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

    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].

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

    Clinical Trial
    Molecular Weight

    429.90

    Formula

    C22H24ClN3O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 5 mg/mL (11.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3261 mL 11.6306 mL 23.2612 mL
    5 mM 0.4652 mL 2.3261 mL 4.6522 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 0.5 mg/mL (1.16 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 0.5 mg/mL (1.16 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.93%

    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 Hydrochloride (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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3261 mL 11.6306 mL 23.2612 mL 58.1531 mL
    5 mM 0.4652 mL 2.3261 mL 4.6522 mL 11.6306 mL
    10 mM 0.2326 mL 1.1631 mL 2.3261 mL 5.8153 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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