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

CFI-402257 hydrochloride 

Cat. No.: HY-101340A Purity: 99.48%
Handling Instructions

CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. 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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 388 In-stock
Estimated Time of Arrival: December 31
1 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 330 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of CFI-402257 hydrochloride:

Top Publications Citing Use of Products

Publications Citing Use of MCE CFI-402257 hydrochloride

    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

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity[1].

    IC50 & Target

    IC50: 1.7 nM (TTK in vitro)[1].

    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].
    CFI-402257 exhibits effects consistent with Mps1 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%.
    Clinical Trial
    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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 125 mg/mL (233.63 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8690 mL 9.3451 mL 18.6902 mL
    5 mM 0.3738 mL 1.8690 mL 3.7380 mL
    10 mM 0.1869 mL 0.9345 mL 1.8690 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (3.89 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (3.89 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (3.89 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Product Name:
    CFI-402257 hydrochloride
    Cat. No.:
    HY-101340A
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