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

Nilotinib monohydrochloride monohydrate (Synonyms: 尼洛替尼盐酸盐一水合物; AMN107 monohydrochloride monohydrate)

目录号: HY-10159A 纯度: 99.89%
产品使用指南

Nilotinib monohydrochloride monohydrate 是一种二代酪氨酸酶抑制剂,有效抑制 BCR-ABL 及其突变体。

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Nilotinib monohydrochloride monohydrate Chemical Structure

Nilotinib monohydrochloride monohydrate Chemical Structure

CAS No. : 923288-90-8

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Other Forms of Nilotinib monohydrochloride monohydrate:

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Top Publications Citing Use of Products

    Nilotinib monohydrochloride monohydrate purchased from MCE. Usage Cited in: Leuk Lymphoma. 2015;56(8):2416-23.

    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.

    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).
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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]

    体外研究
    (In Vitro)

    The novel, selective Abl inhibitor, Nilotinib (AMN107), is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than Imatinib. In addition to being significantly more potent compared with Imatinib (IC50<30 nM), Nilotinib 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. The parent cell lines GK1C and GK3C show Imatinib sensitivity with IC50 of 4.59±0.97 µM and 11.15±1.48 µM, respectively. The Imatinib-resistant cell lines GK1C-IR and GK3C-IR show 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.

    体内研究
    (In Vivo)

    The percentage of tumor growth inhibition (TGI) is 83.8% for Imatinib and 69.6% for Nilotinib in the GK1X xenograft line (n.s.). In the GK2X xenograft line, TGI is 83.0% for Imatinib and 85.3% for Nilotinib (n.s.). Additionally, the GK3X xenograft line TGI is 31.1% for Imatinib and 47.5% for Nilotinib (n.s.). These results suggest that, except for the GK1X xenograft line, Nilotinib shows equivalent or higher antitumor effects than Imatinib[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 Nilotinib decreased the PDGFR α and β levels and apoptotic scores in the colon, it did not have a significant effect on the weight and TNF-α levels. Further experimental investigations could provide more definitive evidence for humans[3].

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

    Clinical Trial
    分子量

    583.99

    Formula

    C28H25ClF3N7O2

    CAS 号
    中文名称

    尼洛替尼盐酸盐一水合物;尼罗替尼盐酸盐一水合物

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO : ≥ 33 mg/mL (56.51 mM)

    H2O : 0.1 mg/mL (0.17 mM; Need ultrasonic)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    参考文献
    Cell Assay
    [2]

    The human GIST cell lines GK1C and GK3C, and the Imatinib-resistant cell lines GK1C-IR and GK3C-IR are plated in 96-well microplates and cultured for 12 h before exposure to Imatinib (1-100 µM) or Nilotinib (1-100 µM) for 72 h. The cells are quantified by the WST-8 assay. The optical density (OD) is determined with Sunrise rainbow. The rate of inhibition is calculated as follows: % of inhibition=(OD of treated group-blank)/(OD of control group-blank)×100%. The concentration of tested drugs resulting in 50% growth inhibition (IC50) is calculated[2].

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

    Animal Administration
    [2][3]

    Mice[2]
    The GIST xenograft lines GK1X, GK2X and GK3X in nude mice are used. These xenograft lines are maintained by continual passage in BALB/cSLc-nu/nu mice. Mice bearing GK1X, GK2X and GK3X tumors (6-8 mice per group) are treated daily with vehicle or 40 mg/kg Imatinib or Nilotinib for 4 weeks. Tumor volume (TV) is determined from caliper measurements of tumor length (L) and width (w) according to the formula LW2/2. TV is determined every two to three days and on the day of evaluation. Mice are sacrificed and the percentage of tumor growth inhibition (TGI) is calculated as follows: TGI (%)=[1-(mean of treatment group tumor volume on evaluation day-mean of treatment group tumor volume on day 1)/(mean of control group tumor volume on evaluation day-mean of control group tumor volume on day 1)]×100.
    Rats[3]
    Female Wistar albino rats, weighing 226-243 g (mean weight, 241.09 g), for use in this study. Nilotinib, administered 20 mg/kg/d in two divided doses, is administered to the Nilotinib group of rats (n=7) for 13 d through an orogastric tube, beginning on the same day as indomethacin administration. Blood and tissue samples for pathological examination are obtained from all rats under ether anesthesia at the end of the 13-d period. All animals are then sacrificed by decapitation.

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

    参考文献
    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    Nilotinib monohydrochloride monohydrate
    目录号:
    HY-10159A
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