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CFI-400945

Name: CFI-400945
Brand: TargetMol
SKU: T22645
Rating: 4.5 (1 reviews)

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Catalog No. T22645Cas No. 1616420-30-4

CFI-400945 is an orally active, potent, and selective inhibitor of polo-like kinase 4.

CFI-400945

😃Good

Catalog No. T22645Cas No. 1616420-30-4

CFI-400945 is an orally active, potent, and selective inhibitor of polo-like kinase 4.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	Inquiry	7-10 days	7-10 days
50 mg	Inquiry	7-10 days	7-10 days
100 mg	Inquiry	7-10 days	7-10 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	CFI-400945 is an orally active, potent, and selective inhibitor of polo-like kinase 4.
Targets&IC50	PLK4:2.8 nM, TRKA:6 nM, TRKB:9 nM, AURKA:140 nM, AURKB/INCENP:98 nM, TIE2/TEK:22 nM
In vitro	In an assay using recombinant human PLK4, CFI-400945 inhibited PLK4 (IC50: 2.8 ± 1.4 nM and Ki: 0.26 ± 0.1 nM in an ATP competitive manner). CFI-400945 inhibited autophosphorylation of PLK4 at serine 305 (EC50: 12.3 nM in cells overexpressing PLK4). CFI-400945 showed no significant inhibitory activity against other PLK family members (PLK1, PLK2, and PLK3 with the IC50s of > 50 μM). In transfected HCT116 cells with TRKA, TRKB, and Tie2/TEK, the EC50 values were 84 nM, 88 nM, and 117 nM, respectively. CFI-400945 inhibited the activity of AURKA and AURKB with the EC50 value of 510 nM and 102 nM. CFI-400945 (≥ 200 nM) decreased the mean centriole number in asynchronous U2OS cells. CFI-400945 inhibited a panel of breast cancer cell growth with the GI50 of 14-165 nM [1].
In vivo	In mice, the maximum tolerated dose (MTD) of CFI-400945 for once-daily oral administration was estimated to be 7.5-9.5 mg/kg [1].

Chemical Properties

Molecular Weight	650.72
Formula	C₃₇H₃₈N₄O₇
Cas No.	1616420-30-4
Smiles	C(=C/C(O)=O)\C(O)=O.O=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.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 10 mg/mL (15.37 mM), Sonication is recommended.

Ethanol: ≤12 mg/mL, Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (1.54 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5368 mL	7.6838 mL	15.3676 mL	76.8380 mL
5 mM	0.3074 mL	1.5368 mL	3.0735 mL	15.3676 mL
10 mM	0.1537 mL	0.7684 mL	1.5368 mL	7.6838 mL

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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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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