1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. Bcr-Abl
    Autophagy
  3. Nilotinib monohydrochloride monohydrate

Nilotinib monohydrochloride monohydrate  (Synonyms: AMN107 monohydrochloride monohydrate)

Cat. No.: HY-10159A Purity: 99.89%
COA Handling Instructions

Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.

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

Nilotinib monohydrochloride monohydrate Chemical Structure

Nilotinib monohydrochloride monohydrate Chemical Structure

CAS No. : 923288-90-8

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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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Estimated Time of Arrival: December 31
Solid
100 mg USD 60 In-stock
Estimated Time of Arrival: December 31
200 mg USD 74 In-stock
Estimated Time of Arrival: December 31
500 mg USD 144 In-stock
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Customer Review

Based on 28 publication(s) in Google Scholar

Other Forms of Nilotinib monohydrochloride monohydrate:

Top Publications Citing Use of Products

    Nilotinib monohydrochloride monohydrate purchased from MCE. 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.

    Nilotinib monohydrochloride monohydrate purchased from MCE. 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).
    • Biological Activity

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    Description

    Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.

    IC50 & Target

    Bcr-Abl[1]

    In Vitro

    Nilotinib (AMN107) monohydrochloride monohydrate, 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 monohydrochloride monohydrate 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].

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

    In Vivo

    Nilotinib monohydrochloride monohydrate (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 monohydrochloride monohydrate 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].

    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

    583.99

    Formula

    C28H25ClF3N7O2

    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.[H]Cl.O

    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 : ≥ 33 mg/mL (56.51 mM)

    H2O : < 0.1 mg/mL (ultrasonic) (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7124 mL 8.5618 mL 17.1236 mL
    5 mM 0.3425 mL 1.7124 mL 3.4247 mL
    10 mM 0.1712 mL 0.8562 mL 1.7124 mL
    *Please refer to the solubility information to select the appropriate solvent.
    Purity & Documentation
    References
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    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:
    Nilotinib monohydrochloride monohydrate
    Cat. No.:
    HY-10159A
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