1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Mps1
  3. CFI-402257 hydrochloride

CFI-402257 hydrochloride 

Cat. No.: HY-101340A
Handling Instructions

CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK and Mps1 inhibitor with Kis of 0.1 and 0.09 nM, respectively. CFI-402257 hydrochloride has anti-cancer activity.

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

CFI-402257 hydrochloride Chemical Structure

CFI-402257 hydrochloride Chemical Structure

CAS No. : 1610677-37-6

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1 mg USD 110 Get quote
5 mg USD 330 Get quote
10 mg USD 500 Get quote
50 mg USD 1500 Get quote
100 mg USD 2100 Get quote

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Top Publications Citing Use of Products

    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.
    • Biological Activity

    • Technical Information

    • Purity & Documentation

    • References

    Description

    CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK and Mps1 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
    Molecular Weight

    535.04

    Formula

    C₂₈H₃₁ClN₆O₃

    CAS No.

    1610677-37-6

    SMILES

    C[[email protected]@]1(O)C[[email protected]@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

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    Product Name:
    CFI-402257 hydrochloride
    Cat. No.:
    HY-101340A
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    CFI-402257 hydrochloride

    Cat. No.: HY-101340A