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CFI-402257

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Catalog No. T22289 Copy Product Info
Purity: 99.51%
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CFI-402257 (Luvixasertib) is a highly selective oral TTK (Mps1, Monopolar Spindle 1) kinase inhibitor that potently inhibits TTK kinase activity (Mps1 Ki = 0.09 nM;EC50 = 6.5 nM). It is intended for use in research on hepatocellular carcinoma and breast cancer.
CFI-402257
Cas No. 1610759-22-2
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Pack SizePriceUSA StockGlobal StockQuantity
1 mg$65In StockIn Stock
5 mg$155In StockIn Stock
10 mg$221In StockIn Stock
25 mg$403In StockIn Stock
50 mg$603In StockIn Stock
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.51%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
CFI-402257 (Luvixasertib) is a highly selective oral TTK (Mps1, Monopolar Spindle 1) kinase inhibitor that potently inhibits TTK kinase activity (Mps1 Ki = 0.09 nM;EC50 = 6.5 nM). It is intended for use in research on hepatocellular carcinoma and breast cancer.
Targets & IC50
TTK:1.7 nM, TTK:0.1 nM (Ki), Mps1:0.09 nM (Ki), Mps1:6.5 nM (EC50)
In vitro
Methods: MHCC97L cells were treated with 100 nM CFI-402257 for 72 hours, followed by flow cytometric analysis of DNA content.
Results: CFI-402257 induced a significant increase in the proportion of aneuploid cells. [1]
In vivo
Methods: MHCC97L-luc cells were implanted in BALB/cAnN-nu mice. Treatment commenced 2 weeks post-implantation when tumor formation initiated. CFI-402257 was administered orally via gavage at 30 mg/kg once daily for 4 consecutive weeks.
Results: Tumor volume significantly decreased, and the number of pulmonary metastatic nodules markedly reduced. [1]
Methods: A carotid artery wire injury model was established in C57BL/6 mice via carotid artery wire injury. Treatment commenced postoperatively with oral gavage of CFI-402257 at 30 mg/kg once daily for 28 consecutive days.
Results: The area of newly formed endothelium and the intima-media ratio were significantly reduced, while re-endothelialization remained unaffected (confirmed by CD31 staining), demonstrating superiority over conventional drug-eluting stents. [2]
Chemical Properties
Molecular Weight498.58
FormulaC28H30N6O3
Cas No.1610759-22-2
SmilesN(C[C@H]1C[C@@](C)(O)C1)C=2N3C(=C(C=N3)C4=CC(C)=C(C(NC5CC5)=O)C=C4)N=C(OC=6C=CC=NC6)C2
Relative Density.1.42 g/cm3 (Predicted)
Storage & Solubility Information
StorageStore at low temperature,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 37.7 mg/mL (75.61 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0057 mL10.0285 mL20.0570 mL100.2848 mL
5 mM0.4011 mL2.0057 mL4.0114 mL20.0570 mL
10 mM0.2006 mL1.0028 mL2.0057 mL10.0285 mL
20 mM0.1003 mL0.5014 mL1.0028 mL5.0142 mL
50 mM0.0401 mL0.2006 mL0.4011 mL2.0057 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Keywords

Related Tags: CFI-402257 chemical structure | CFI-402257 in vivo | CFI-402257 in vitro | CFI-402257 formula | CFI-402257 molecular weight