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

CFI-402257 

Cat. No.: HY-101340 Purity: 99.52%
Handling Instructions

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

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

CFI-402257 Chemical Structure

CFI-402257 Chemical Structure

CAS No. : 1610759-22-2

Size Price Stock Quantity
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
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of CFI-402257:

Top Publications Citing Use of Products

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

    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
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 1.67 mg/mL (3.35 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0057 mL 10.0285 mL 20.0570 mL
    5 mM --- --- ---
    10 mM --- --- ---
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Molecular Weight

    498.58

    Formula

    C₂₈H₃₀N₆O₃

    CAS No.

    1610759-22-2

    SMILES

    CC1=CC(C2=C3N=C(OC4=CN=CC=C4)C=C(NC[[email protected]@H]5C[[email protected]@](O)(C)C5)N3N=C2)=CC=C1C(NC6CC6)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.52%

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    CFI-402257
    Cat. No.:
    HY-101340
    Quantity:

    CFI-402257

    Cat. No.: HY-101340