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Ocifisertib(CFI-400945 free base)

🥰Excellent
Catalog No. T7384Cas No. 1338806-73-7

Ocifisertib (CFI-400945 free base) is a potent, selective and orally active inhibitor of polo-like kinase 4 (PLK4; Ki value 0.26 nM; IC50 value 2.8 nM).

Ocifisertib(CFI-400945 free base)

Ocifisertib(CFI-400945 free base)

🥰Excellent
Purity: 99.04%
Catalog No. T7384Cas No. 1338806-73-7
Ocifisertib (CFI-400945 free base) is a potent, selective and orally active inhibitor of polo-like kinase 4 (PLK4; Ki value 0.26 nM; IC50 value 2.8 nM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$38In StockIn Stock
5 mg$88In StockIn Stock
10 mg$143In StockIn Stock
25 mg$295In StockIn Stock
50 mg$513In StockIn Stock
100 mg$818-In Stock
1 mL x 10 mM (in DMSO)$98In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.04%
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Product Introduction

Bioactivity
Description
Ocifisertib (CFI-400945 free base) is a potent, selective and orally active inhibitor of polo-like kinase 4 (PLK4; Ki value 0.26 nM; IC50 value 2.8 nM).
Targets&IC50
PLK4:0.26 nM(Ki), TRKA:6 nM, TIE2/TEK:22 nM, AURKB/INCENP:98 nM, AURKA:140 nM, TRKB:9 nM
In vitro
METHODS: HCT116 cells with FLAG-tagged full-length PLK4 were treated with Ocifisertib (CFI-400945 free base) for 4 hours, and the lysates were analyzed by immunoblotting.
RESULTS In cells overexpressing PLK4, Ocifisertib inhibited PLK4 autophosphorylation at serine 305 with an EC50 value of 12.3 nM.[1]
In vivo
METHODS: PK analysis was performed in mice treated with ocifisertib (CFI-400945 free base) (3.75-104 mg/kg, oral).
RESULTS CFI-400945 was rapidly absorbed after oral administration, reaching maximum plasma concentrations (Cmax) of 0.25–11.68 μg/mL; the elimination half-life was 3.7-4.2 hours at 3.75-26 mg/kg, but was prolonged with increasing doses (5.4 and 6.9 hours at 52 and 104 mg/kg, respectively). [1]
Chemical Properties
Molecular Weight534.65
FormulaC33H34N4O3
Cas No.1338806-73-7
SmilesO=C1[C@]2([C@@H](C2)C=3C=C4C(=CC3)C(/C=C/C5=CC=C(CN6C[C@@H](C)O[C@@H](C)C6)C=C5)=NN4)C=7C(N1)=CC=C(OC)C7
Relative Density.1.32 g/cm3 (Predicted)
ColorYellow
AppearanceSolid
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 100 mg/mL (187.04 mM), Sonication is recommended.
H2O: Insoluble
DMSO: 100 mg/mL (187.04 mM), Heating to 50℃ is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7.48 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM1.8704 mL9.3519 mL18.7038 mL93.5191 mL
5 mM0.3741 mL1.8704 mL3.7408 mL18.7038 mL
10 mM0.1870 mL0.9352 mL1.8704 mL9.3519 mL
20 mM0.0935 mL0.4676 mL0.9352 mL4.6760 mL
50 mM0.0374 mL0.1870 mL0.3741 mL1.8704 mL
100 mM0.0187 mL0.0935 mL0.1870 mL0.9352 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
1 Enter information below:
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2 Enter the in vivo formulation:
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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