Luvixasertib
Based on 7 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.9600%
- CAS. Nr.: 1610759-22-2
- Formel: C28H30N6O3
- Molecular Weight:498.58
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) Luvixasertib
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Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 1.7 nM (TTK in vitro)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HeLa | IC50 |
116 nM
Compound: 86; CFI-402257
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Inhibition of MPS1 in human HeLa cells assessed as reduction in spindle assembly checkpoint incubated for 4 hrs by p-histone H3/Hoechst 33342 staining based microscopic analysis
Inhibition of MPS1 in human HeLa cells assessed as reduction in spindle assembly checkpoint incubated for 4 hrs by p-histone H3/Hoechst 33342 staining based microscopic analysis
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[PMID: 32338514] |
| HT-29 | IC50 |
557 nM
Compound: 86; CFI-402257
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Antiproliferative activity against human HT-29 cells after 96 hrs by crystal violet staining based assay
Antiproliferative activity against human HT-29 cells after 96 hrs by crystal violet staining based assay
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[PMID: 32338514] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells.
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Concentration:0 nM, 50 nM, 100 nM, 300 nM, 1000 nM, 3000 nM.
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Incubation Time:48 hours.
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Result:Resulted in an increase in the frequency of cells exhibiting an aneuploid DNA content.
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Cell Line:HCT116 cells.
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Concentration:0 nM, 50 nM or 100 nM.
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Incubation Time:8, 16, 24 and 48 hours.
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Xenografted MDA-MB-231 human TNBC cells and MDA-MB-468 human TNBC cells in mice[2].
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Dosage:5, 6 mg/kg.
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Administration:Oral gavage, daily.
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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%.
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Animal Model:PDX model of high-grade serous ovarian cancer[2].
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Dosage:6.5, 7.5 mg/kg.
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Administration:Oral gavage, daily.
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Result:6.5 mg/kg, tumor growth inhibition (TGI) = 61%; 7.5 mg/kg, TGI = 97%.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1610759-22-2
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Appearance Solid
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Molecular Weight 498.58
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Formel C28H30N6O3
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Color White to off-white
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SMILES
CC1=CC(C2=C3N=C(OC4=CN=CC=C4)C=C(NC[C@@H]5C[C@@](O)(C)C5)N3N=C2)=CC=C1C(NC6CC6)=O
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Synonyms
CFI-402257
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (7)
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Journal Impact Factor
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Most Recent
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Cancer Discov
Cells Lacking the RB1 Tumor Suppressor Gene Are Hyperdependent on Aurora B Kinase for Survival. [Abstract]2019 Feb;9(2):230-247. PMID: 30373918
Luvixasertib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2019 Feb;9(2):230-247. [Abstract]
Western analysis of protein expression in different concentrations of CFI-402257 treatment.
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Commun Biol
Integrated genomics and comprehensive validation reveal drivers of genomic evolution in esophageal adenocarcinoma. [Abstract]2021 May 24;4(1):617. PMID: 34031527 -
Oncol Rep
Energy‑stress‑mediated activation of AMPK sensitizes MPS1 kinase inhibition in triple‑negative breast cancer. [Abstract]2024 Aug;52(2):101. PMID: 38904203 -
PLoS Genet
Barrier-to-autointegration factor protects against the cGAS-STING response to chromatin bridges. [Abstract]2026 Jun 3;22(6):e1012191. PMID: 42234713 -
Front Oncol
Dual TTK/PLK1 inhibition has potent anticancer activity in TNBC as monotherapy and in combination. [Abstract]2024 Aug 9:14:1447807. PMID: 39184047 -
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Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 1.67 mg/mL (3.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Liu Y, et al. Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent. ACS Med Chem Lett. 2016 May 6;7(7):671-5. [Content Brief]
[2]. Mason JM, et al. Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3127-3132. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.0057 mL | 10.0285 mL | 20.0570 mL | 50.1424 mL |
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