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

Neratinib  (Synonyms: HKI-272)

Cat. No.: HY-32721 Purity: 99.59%
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Neratinib (HKI-272) 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 Chemical Structure

Neratinib Chemical Structure

CAS No. : 698387-09-6

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10 mM * 1 mL in DMSO
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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of Neratinib:

Top Publications Citing Use of Products

    Neratinib 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 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.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target[1]

    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.

    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

    557.04

    Formula

    C30H29ClN6O3

    CAS No.
    Appearance

    Solid

    Color

    White to light brown

    SMILES

    ClC1=C(OCC2=NC=CC=C2)C=CC(NC3=C(C#N)C=NC4=CC(OCC)=C(NC(/C=C/CN(C)C)=O)C=C43)=C1

    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 : 13.33 mg/mL (23.93 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7952 mL 8.9760 mL 17.9520 mL
    5 mM 0.3590 mL 1.7952 mL 3.5904 mL
    10 mM 0.1795 mL 0.8976 mL 1.7952 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  0.5% MC  0.5% Tween-80

      Solubility: 3.33 mg/mL (5.98 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: 2 mg/mL (3.59 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 0.83 mg/mL (1.49 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.59%

    References
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    Neratinib 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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    Product Name:
    Neratinib
    Cat. No.:
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