2. Protein Tyrosine Kinase/RTK Autophagy
  3. Bcr-Abl Autophagy
  4. Nilotinib

Nilotinib  (Synonyms: AMN107)

Cat. No.: HY-10159 Purity: 99.93%
COA Handling Instructions

Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.

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

Nilotinib Chemical Structure

Nilotinib Chemical Structure

CAS No. : 641571-10-0

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10 mM * 1 mL in DMSO
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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Nilotinib:

Nilotinib Related Antibodies

Top Publications Citing Use of Products

    Nilotinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Apr 24;9(31):22158-22183.  [Abstract]

    Primary tumors are dissected at the end of experiment and subjected to immunohistochemistry. Representative images of primary tumor sections stained with anti-PCNA (proliferation), anti-cleaved caspase 3 (apoptosis), and anti-CD31 (angiogenesis).

    Nilotinib purchased from MedChemExpress. Usage Cited in: Leuk Lymphoma. 2015;56(8):2416-23.  [Abstract]

    Cell cycle analysis of HT93A cells by flow cytometry. Cells are treated with 100 nM Nilotinib and 50 ng/mL G-CSF alone or in combination for 48 h before the cell cycle is analyzed. Nilotinib treatment increases the fraction of cells in G0/G1 phase and decreased the S+G2/M-phase fraction.

    • Biological Activity

    • Purity & Documentation

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    • Customer Review

    Description

    Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.

    IC50 & Target

    Bcr-Abl[1]
    In Vitro

    Nilotinib (AMN107), selective Abl inhibitor, is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than imatinib while being significantly more potent compared with imatinib (IC50<30 nM), also maintains activity against most of the BCR-ABL point mutants that confer Imatinib resistance[1].
    Nilotinib demonstrates significant antitumor efficacy against GIST xenograft lines and imatinib-resistant GIST cell lines which parent cell lines GK1C and GK3C shows imatinib sensitivity with IC50 of 4.59±0.97 µM and 11.15±1.48 µM, respectively, imatinib-resistant cell lines GK1C-IR and GK3C-IR shows Imatinib resistance with IC50 values of 11.74±0.17 µM (P<0.001) and 41.37±1.07 µM (P<0.001), respectively[2].

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

    Nilotinib Related Antibodies
    In Vivo

    Nilotinib (oral gavage, 40 mg/kg, daily, 4 weeks) shows equivalent or higher antitumor effects in BALB/cSLc-nu/nu mice with GIST xenograft[2].
    Nilotinib has a significant healing effect on the macroscopic and microscopic pathologic scores and ensures considerable mucosal healing in the indomethacin-induced enterocolitis rat model while decreases the PDGFR α and β levels and apoptotic scores in the colon[3].

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

    Animal Model: BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X)[2]
    Dosage: 40 mg/kg
    Administration: Oral gavage; daily; 4 weeks
    Result: Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X and 47.5% in GK3X xenograft line.
    Clinical Trial
    Molecular Weight

    529.52

    Appearance

    Solid

    Formula

    C28H22F3N7O
    CAS No.
    SMILES

    O=C(NC1=CC(C(F)(F)F)=CC(N2C=NC(C)=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=CC=CN=C5)=N4)=C3
    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 : 12.5 mg/mL (23.61 mM; ultrasonic and warming and heat to 60°C)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8885 mL 9.4425 mL 18.8850 mL
    5 mM 0.3777 mL 1.8885 mL 3.7770 mL
    10 mM 0.1889 mL 0.9443 mL 1.8885 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 0.5 mg/mL (0.94 mM); Clear solution

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

    Purity: 99.93%

    COA (245 KB) HNMR (187 KB) LCMS (444 KB)

    Handling Instructions (2659 KB)
    References
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    Nilotinib 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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    Keywords:

    Nilotinib641571-10-0AMN107AMN 107AMN-107Bcr-AblAutophagytyrosine kinaseantitumorInhibitorinhibitorinhibit

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