2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Olmutinib

Olmutinib  (Synonyms: HM61713; BI 1482694)

Cat. No.: HY-19730 Purity: 99.68%
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Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC.

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

Olmutinib Chemical Structure

Olmutinib Chemical Structure

CAS No. : 1353550-13-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
1 mg USD 26 In-stock
5 mg USD 66 In-stock
10 mg USD 106 In-stock
50 mg USD 238 In-stock
100 mg USD 370 In-stock
200 mg USD 594 In-stock
500 mg   Get quote  
1 g   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Olmutinib:

Olmutinib Related Antibodies

Top Publications Citing Use of Products

    Olmutinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2018 Jul;8(4):563-574.  [Abstract]

    The protein levels of ABCG2 in MDR cells after different concentrations Olmutinib stimulation for 48 h are measured by Western blot analysis (GAPDH as loading control).

    View All EGFR Isoform Specific Products:

    View All Isoforms
    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC[1][2].

    IC50 & Target[1]

    EGFRExon 19 deletion

    9.2 nM (IC50, Cell Assay)

    EGFRL858R/T790M

    10 nM (IC50, Cell Assay)

    In Vitro

    Olmutinib potently inhibits EGFR in HCC827 cells expressing EGFRDEL19 (IC50=9.2 nM) and H1975 cells expressing EGFRL858R/T790M (IC50=10 nM). In contrast, the IC50 of olmutinib against cells expressing EGFRWT is 2225 nM[1].

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

    Olmutinib Related Antibodies
    Clinical Trial
    Molecular Weight

    486.59

    Formula

    C26H26N6O2S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    C=CC(NC1=CC=CC(OC2=C3C(C=CS3)=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (256.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0551 mL 10.2756 mL 20.5512 mL
    5 mM 0.4110 mL 2.0551 mL 4.1102 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    • Dilution Calculator

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

    Mass
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    Volume
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    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: ≥ 6.25 mg/mL (12.84 mM); Clear solution

      This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: 6.25 mg/mL (12.84 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 6.25 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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).
    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
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0551 mL 10.2756 mL 20.5512 mL 51.3780 mL
    5 mM 0.4110 mL 2.0551 mL 4.1102 mL 10.2756 mL
    10 mM 0.2055 mL 1.0276 mL 2.0551 mL 5.1378 mL
    15 mM 0.1370 mL 0.6850 mL 1.3701 mL 3.4252 mL
    20 mM 0.1028 mL 0.5138 mL 1.0276 mL 2.5689 mL
    25 mM 0.0822 mL 0.4110 mL 0.8220 mL 2.0551 mL
    30 mM 0.0685 mL 0.3425 mL 0.6850 mL 1.7126 mL
    40 mM 0.0514 mL 0.2569 mL 0.5138 mL 1.2844 mL
    50 mM 0.0411 mL 0.2055 mL 0.4110 mL 1.0276 mL
    60 mM 0.0343 mL 0.1713 mL 0.3425 mL 0.8563 mL
    80 mM 0.0257 mL 0.1284 mL 0.2569 mL 0.6422 mL
    100 mM 0.0206 mL 0.1028 mL 0.2055 mL 0.5138 mL
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    Olmutinib Related Classifications

    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.

    Keywords:

    Olmutinib1353550-13-6HM61713 BI 1482694HM 61713HM-61713BI1482694BI 1482694BI-1482694EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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