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  1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Mps1

CFI-402257 hydrochloride 

目录号: HY-101340A
产品使用指南

CFI-402257 hydrochloride 是高度选选择性,具有口服活性的 TTKMps1抑制剂,Ki值分别为 0.1 nM和 0.09 nM。CFI-402257 hydrochloride 具有抗癌活性。

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CFI-402257 hydrochloride Chemical Structure

CFI-402257 hydrochloride Chemical Structure

CAS No. : 1610677-37-6

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CFI-402257 hydrochloride 的其他形式现货产品:

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的科研文献

Cancer Discov. 2019 Feb;9(2):230-247.

    CFI-402257 hydrochloride purchased from MCE. Usage Cited in: Cancer Discov. 2019 Feb;9(2):230-247.

    Western analysis of protein expression in different concentrations of CFI-402257 treatment.
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    • 参考文献

    Description

    CFI-402257 hydrochloride is a highly selective and orally bioavailable TTKandMps1 inhibitor with Kis of 0.1 and 0.09 nM, respectively. CFI-402257 hydrochloride has anti-cancer activity[1].

    IC50 & Target

    Ki: 0.1 nM (TTK)[1], 0.09 nM (Mps1)[2]
    EC50: 6.5 nM (Mps1)[2].

    In Vitro

    CFI-402257 is highly selective to TTK. CFI-402257 is tested against a panel of human kinases at 1 μM and inhibits none of the 262 kinases tested. CFI-402257 is a potent inhibitor of cell growth[1].
    CFI-402257 (200 nM, 6 h) causes a massive increase in chromosome missegregations[2].
    CFI-402257 (0, 50 or 100 nM) induces a dose-dependent dysregulation of the cell cycle, resulting in an increase in the frequency of cells exhibiting an aneuploid DNA content[2].
    All in all, CFI-402257 exhibit effects consistent withMps1 kinase inhibition, specifically SAC inactivation, leading to chromosome missegregation, aneuploidy, and ultimately cell death[2].

    Cell Cycle Analysis[2]

    Cell Line:HCT116 cells.
    Concentration:0 nM, 50 nM, 100 nM, 300 nM, 1000 nM, 3000 nM.
    Incubation Time:48 hours
    Result:Resulted in an increase in the frequency of cells exhibiting an aneuploid DNA content.

    Western Blot Analysis[2]

    Cell Line:HCT116 cells.
    Concentration:0 nM, 50 nM or 100 nM.
    Incubation Time:8, 16, 24 and 48 hours.
    Result:CFI-402257-induced aneuploidy was accompanied by a progressive accumulation of apoptotic cells that were detectable as early as 16 h following treatment.
    In Vivo

    CFI-402257 given orally QD shows dose-dependent activity in mice with established tumors from xenografted MDA-MB-231 human TNBC cells and MDA-MB-468 human TNBC cells in mice. CFI-402257 demonstrates antitumor activity in a platinum-resistant PDX model of high-grade serous ovarian cancer[2].

    Animal Model:Xenografted MDA-MB-231 human TNBC cells and MDA-MB-468 human TNBC cells in mice[2].
    Dosage:5, 6 mg/kg.
    Administration:Oral gavage, daily.
    Result:Xenografted MDA-MB-231 human TNBC cells: 5 mg/kg, tumor growth inhibition (TGI) = 74%; 6 mg/kg, TGI = 89%.
    Xenografted MDA-MB-468 human TNBC cells: 5 mg/kg, tumor growth inhibition (TGI) = 75%; 6 mg/kg, TGI = 94%.
    Animal Model:PDX model of high-grade serous ovarian cancer[2].
    Dosage:6.5, 7.5 mg/kg.
    Administration:Oral gavage, daily.
    Result:6.5 mg/kg, tumor growth inhibition (TGI) = 61%; 7.5 mg/kg, TGI = 97%.
    References
    • [1].Liu Y, et al. Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent. ACS Med Chem Lett. 2016 May 6;7(7):671-5.

      [2].Mason JM, et al. Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3127-3132.

    Molecular Weight

    535.04

    Formula

    C₂₈H₃₁ClN₆O₃

    CAS No.

    1610677-37-6

    SMILES

    C[C@@]1(O)C[C@@H](C1)CNC2=CC(OC3=CN=CC=C3)=NC4=C(C5=CC(C)=C(C(NC6CC6)=O)C=C5)C=NN24.[H]Cl

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    • [1].Liu Y, et al. Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent. ACS Med Chem Lett. 2016 May 6;7(7):671-5.

      [2].Mason JM, et al. Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3127-3132.

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    ×=×
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    产品名称:
    CFI-402257 hydrochloride
    目录号:
    HY-101340A
    需求量:

    CFI-402257 hydrochloride

    Cat. No.: HY-101340A