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

Falnidamol  (Synonyms: BIBX 1382)

Cat. No.: HY-10322 Purity: 99.05%
COA Handling Instructions

Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.

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

Falnidamol Chemical Structure

Falnidamol Chemical Structure

CAS No. : 196612-93-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 131 In-stock
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10 mg USD 211 In-stock
50 mg USD 726 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Falnidamol purchased from MedChemExpress. Usage Cited in: Neuroscience. 2015 Jul 20;304:109-121.  [Abstract]

    GluN2B Y1472 phosphorylation in whole-cell lysate is increased after 5 and 10 min of EGF treatment in cultured neurons which could be blocked by BIBX-1382. EGFR activation increases SFK activity and phosphorylation of GluN2B Y1472. (A) Representative Western blot result of whole lysate samples from hippocampal slices treated with 50 ng/mL EGF incubation for 10 min. (B) Western blot of EGFR-treated DIV14 cultured hippocampal neurons with minimum glia composition shows increased phosphorylation of
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity[1][2].

    IC50 & Target[1]

    EGFR

    3 nM (IC50)

    ErbB2

    3.4 μM (IC50)

    In Vitro

    Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells[2].

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

    In Vivo

    Falnidamol (BIBX 1382; p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment[2].
    Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice[2].
    With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C4h is 2222 nM and the C24h is 244 nM[2].

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

    Animal Model: Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells[2]
    Dosage: 10 mg/kg
    Administration: p.o.; daily; 16 days
    Result: Completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment.
    Animal Model: Five- to six-week-old athymic NMRI-nu/nu female mice (21–31 g) with A431 cells[2]
    Dosage: 10 mg/kg (Pharmacokinetic Analysis)
    Administration: p.o.; daily; 16 days
    Result: The C4h is 2222 nM and the C24h is 244 nM.
    Clinical Trial
    Molecular Weight

    387.84

    Formula

    C18H19ClFN7

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to khaki

    SMILES

    ClC1=CC(NC2=NC=NC3=CN=C(NC(CC4)CCN4C)N=C23)=CC=C1F

    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 : 31.25 mg/mL (80.57 mM; ultrasonic and warming and heat to 60°C; 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 2.5784 mL 12.8919 mL 25.7838 mL
    5 mM 0.5157 mL 2.5784 mL 5.1568 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

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    C2

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    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: ≥ 1.67 mg/mL (4.31 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
    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

    Purity: 99.05%

    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 2.5784 mL 12.8919 mL 25.7838 mL 64.4596 mL
    5 mM 0.5157 mL 2.5784 mL 5.1568 mL 12.8919 mL
    10 mM 0.2578 mL 1.2892 mL 2.5784 mL 6.4460 mL
    15 mM 0.1719 mL 0.8595 mL 1.7189 mL 4.2973 mL
    20 mM 0.1289 mL 0.6446 mL 1.2892 mL 3.2230 mL
    25 mM 0.1031 mL 0.5157 mL 1.0314 mL 2.5784 mL
    30 mM 0.0859 mL 0.4297 mL 0.8595 mL 2.1487 mL
    40 mM 0.0645 mL 0.3223 mL 0.6446 mL 1.6115 mL
    50 mM 0.0516 mL 0.2578 mL 0.5157 mL 1.2892 mL
    60 mM 0.0430 mL 0.2149 mL 0.4297 mL 1.0743 mL
    80 mM 0.0322 mL 0.1611 mL 0.3223 mL 0.8057 mL
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    Falnidamol 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.

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