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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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 66 In-stock
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200 mg USD 74 In-stock
500 mg USD 144 In-stock
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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Nilotinib monohydrochloride monohydrate:

Top Publications Citing Use of Products
Proliferation Assay
IHC

    Nilotinib monohydrochloride monohydrate 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 monohydrochloride monohydrate 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

    • References

    • Customer Review

    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].

    MedChemExpress (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].

    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

    583.99

    Formula

    C28H25ClF3N7O2

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    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 : 33.33 mg/mL (57.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    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
    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

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

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    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 1.7124 mL 8.5618 mL 17.1236 mL 42.8090 mL
    5 mM 0.3425 mL 1.7124 mL 3.4247 mL 8.5618 mL
    10 mM 0.1712 mL 0.8562 mL 1.7124 mL 4.2809 mL
    15 mM 0.1142 mL 0.5708 mL 1.1416 mL 2.8539 mL
    20 mM 0.0856 mL 0.4281 mL 0.8562 mL 2.1404 mL
    25 mM 0.0685 mL 0.3425 mL 0.6849 mL 1.7124 mL
    30 mM 0.0571 mL 0.2854 mL 0.5708 mL 1.4270 mL
    40 mM 0.0428 mL 0.2140 mL 0.4281 mL 1.0702 mL
    50 mM 0.0342 mL 0.1712 mL 0.3425 mL 0.8562 mL
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    Nilotinib monohydrochloride monohydrate 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:
    Nilotinib monohydrochloride monohydrate
    Cat. No.:
    HY-10159A
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