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CFI-402257

Cat. No. M6078
CFI-402257 Structure
Size Price Availability
5mg USD 350 4-7 Days
10mg USD 550 4-7 Days
50mg USD 1500 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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. CFI-402257 shows strong antineoplastic activity on a broad panel of human cancer-derived cell lines, and causes effects consistent with depletion or inhibition of Mps1. CFI-402257 inhibits Mps1 with an IC50 value of 1.2 nM, and is ATP competitive with a Ki value of 0.09 nM. CFI-402257 inhibits autophosphorylation of Mps1 at threonine 12/serine 15 with an EC50 value of 6.5 nM in cells exogenously expressing human Mps1. CFI-402257 exerts potent growth inhibitory activity across the vast majority of cell lines with a median IC50 value of 15 nM. In vivo: The upper dose level for once-daily administration of CFI-402257 is between 6 and 6.5 mg/kg. CFI-402257 given orally QD shows dose-dependent activity in mice with established tumors from xenografted MDA-MB-231 human TNBC cells [5 mg/kg CFI-402257, tumor growth inhibition (TGI)=74%; 6 mg/kg, TGI=89%], from xenografted MDA-MB-468 human TNBC cells in mice (5 mg/kg, TGI=75%; 6 mg/kg, TGI=94%). CFI-402257 also demonstrates antitumor activity in a platinum-resistant PDX model of high-grade serous ovarian cancer (6.5 mg/kg, TGI=61%). CFI-402257 is found to be similarly efficacious in a platinum-sensitive PDX model of high-grade serous ovarian cancer.

Protocol
Cell Experiment
Cell lines HCT116 cells
Preparation method Cells were pretreated with 0.5 μM MG132 for 30 min before treatment with CFI-402257 or DMSO for 4 h. For cellular histone H3 (S10) EC50 determination, HCT116 cells were treated with 200 ng/mL nocodazole for 17 h before treatment with CFI-402257 or DMSO for 4 h.
Concentrations 10 μM
Incubation time 17 h
Animal Experiment
Animal models CD-1 nude mice
Formulation 10% (vol/vol) NMP/40% (vol/vol) PEG-300/50% (vol/vol) water
Dosages 10, 25, and 55 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 498.58
Formula C28H30N6O3
CAS Number 1610759-22-2
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
References

Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer.
Mason JM, et al. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3127-3132. PMID: 28270606.

Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent.
Liu Y, et al. ACS Med Chem Lett. 2016 May 6;7(7):671-5. PMID: 27437075.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CFI-402257 supplier, inhibitors

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