All AbMole products are for research use only, cannot be used for human consumption.
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.
Cancer Res. 2024 Mar 22.
Spindle assembly checkpoint as a therapeutic target for TP53-mutated myeloid neoplasms
CFI-402257 purchased from AbMole
| 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 |
| Molecular Weight | 498.58 |
| Formula | C28H30N6O3 |
| CAS Number | 1610759-22-2 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Products |
|---|
| Lactate calcium
Lactate calcium is an excellent calcium fortifier that works better than inorganic calcium. Lactate calcium is used as an antacid. |
| Coniferyl ferulate
Coniferyl ferulate is a potent glutathione S-transferase (GST) inhibitor that reverses multidrug resistance and down-regulates p-glycoprotein. Coniferyl ferulate strongly inhibited human placental glutathione S-transferase with IC50 of 0.3 μM. |
| NXY-059
NXY-059 is a free radical-trapping neuroprotectant that has been reported to reduce infarct size and preserve brain function in experimental models of acute ischemic stroke. |
| Tie2 kinase inhibitor
Tie2 kinase inhibitor is a potent, reversible, and ATP-binding site-targeting Tie2 inhibitor with an IC50 of 250 nM. |
| Calcium levofolinate
Calcium levofolinate is a calcium salt of folinic acid that is an adjuvant used in cancer chemotherapy. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
