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

Neratinib maleate  (Synonyms: HKI-272 maleate)

Cat. No.: HY-32721B Purity: 99.83%
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Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.

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

Neratinib maleate Chemical Structure

Neratinib maleate Chemical Structure

CAS No. : 915942-22-2

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Based on 21 publication(s) in Google Scholar

Other Forms of Neratinib maleate:

Neratinib maleate Related Antibodies

Top Publications Citing Use of Products

    Neratinib maleate purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2018 Jun 20;10(446):eaao2565.  [Abstract]

    Immunoblots of 3 individual KM tumors from mice treated for 3 days with Neratinib or vehicle control.

    Neratinib maleate purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Apr;109(4):1166-1176.  [Abstract]

    Influence of BIBW 2992 or Neratinib on human epidermal growth factor receptor 2 (HER2) and the downsignal pathway in gastric cancer cell lines.

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    Description

    Neratinib (HKI-272) maleate is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively[1].

    IC50 & Target

    HER2

    59 nM (IC50)

    EGFR

    92 nM (IC50)

    In Vitro

    Neratinib displays no activity against other serine-threonine kinases such as Akt, cyclin D1/cdk4, cyclin E/cdk2, cyclin B1/cdk1, IKK-2, MK-2, PDK1, c-Raf, and Tpl-2, as well as the tyrosine kinase c-Met[1].
    Neratinib (0.5 ng/mL–5 μg/mL, 2 days) inhibits the proliferation of cell lines that show high levels of HER-2 (3T3/neu, SK-Br-3, and BT474) and is much less active in cell lines that express neither HER-2 nor EGFR (3T3, MDA-MB-435, and SW620) [1].
    Neratinib (0-2 nM, 12-16 h) arrests BT474 cell cycle at G1-S phase[1].
    Neratinib results in the inhibition of MAPK and Akt phosphorylation, down-regulation of cyclin D1 levels, and induction of p27[1].

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

    Neratinib maleate Related Antibodies

    Cell Proliferation Assay[1]

    Cell Line: 3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620
    Concentration: 0.5 ng/mL–5 μg/mL
    Incubation Time: 2 days (6 days for BT474)
    Result: Inhibited cell proliferation with IC50 values of 700 ± 78, 3 ± 0.14, 2 ± 0.18, 2 ± 0.06, 81± 9, 960 ± 165 and 690 ± 84 nM against 3T3, 3T3/neu, SK-Br-3, BT 474, A431, MDA-MB-435 and SW620 cells, respectively.

    Western Blot Analysis[1]

    Cell Line: BT474 or A431 cells
    Concentration: 0, 2, 10, 50, 100 and 200 nM
    Incubation Time: 3 h
    Result: Decreased ligand-independent receptor phosphorylation by 50% (IC50) at 5 nM in BT474 cells, repressed EGF-dependent phosphorylation of EGFR in A431 cells at a comparable dose (IC50 = 3 nM).
    Effectively repressed phosphorylation of MAPK and Akt in BT474 cells.

    Cell Cycle Analysis[1]

    Cell Line: BT474
    Concentration: 0–2 nM
    Incubation Time: 12–16 h
    Result: Blocked cell cycle progression, causing a G1-S arrest, a 50% decrease in the number of cells in the S (DNA synthesis) phase of the cell cycle was observed at a concentration of 2 nM.
    In Vivo

    Neratinib (HKI-272) (0-80 mg/kg/day; i.g.; 42 days) shows anticancer activities against cancer cells that expresses high levels of HER-2 or EGFR[1].

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

    Animal Model: Female athymic (nude) mice, tumor xenograft[1]
    Dosage: 10, 20, 40, 60 or 80 mg/kg/day
    Administration: Gavage, 42 days
    Result: Reduced tumor growth in a dose-dependent manner in 3T3/neu, BT474, SK-OV-3 and A431 xenografts, but was o inactive in xenografts of MX-1 and MCF-7. Inhibited phosphorylation of HER-2 in BT474 xenografts.
    Clinical Trial
    Molecular Weight

    673.11

    Formula

    C34H33ClN6O7
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC(/C=C\C(O)=O)=O.CCOC(C(NC(/C=C/CN(C)C)=O)=C1)=CC2=C1C(NC3=CC(Cl)=C(C=C3)OCC4=CC=CC=N4)=C(C#N)C=N2
    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 : 250 mg/mL (371.41 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 1.4856 mL 7.4282 mL 14.8564 mL
    5 mM 0.2971 mL 1.4856 mL 2.9713 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.

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Dosing volume
    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    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, 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 1.4856 mL 7.4282 mL 14.8564 mL 37.1410 mL
    5 mM 0.2971 mL 1.4856 mL 2.9713 mL 7.4282 mL
    10 mM 0.1486 mL 0.7428 mL 1.4856 mL 3.7141 mL
    15 mM 0.0990 mL 0.4952 mL 0.9904 mL 2.4761 mL
    20 mM 0.0743 mL 0.3714 mL 0.7428 mL 1.8571 mL
    25 mM 0.0594 mL 0.2971 mL 0.5943 mL 1.4856 mL
    30 mM 0.0495 mL 0.2476 mL 0.4952 mL 1.2380 mL
    40 mM 0.0371 mL 0.1857 mL 0.3714 mL 0.9285 mL
    50 mM 0.0297 mL 0.1486 mL 0.2971 mL 0.7428 mL
    60 mM 0.0248 mL 0.1238 mL 0.2476 mL 0.6190 mL
    80 mM 0.0186 mL 0.0929 mL 0.1857 mL 0.4643 mL
    100 mM 0.0149 mL 0.0743 mL 0.1486 mL 0.3714 mL
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    Neratinib maleate Related Classifications

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    • 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:

    Neratinib915942-22-2HKI-272HKI272HKI 272EGFREpidermal growth factor receptorErbB-1HER1breast cancersolid tumorsnon–small-cell lung cancerBT474A431gastric cancerInhibitorinhibitorinhibit

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