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

Falnidamol (Synonyms: BIBX 1382)

Cat. No.: HY-10322 Purity: 98.07%
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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10 mM * 1 mL in DMSO USD 131 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Falnidamol purchased from MCE. Usage Cited in: Neuroscience. 2015 Jul 20;304:109-121.

    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
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    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].

    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].

    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.

    196612-93-8

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 41 mg/mL (105.71 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.2578 mL 1.2892 mL 2.5784 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: ≥ 1.67 mg/mL (4.31 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    FalnidamolBIBX 1382BIBX1382BIBX-1382EGFREpidermal growth factor receptorErbB-1HER1Orallytyrosinekinasepyrimido-pyrimidineanti-cancerInhibitorinhibitorinhibit

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