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PF-2771

Name: PF-2771
Brand: TargetMol
SKU: T12434
Rating: 4.5 (1 reviews)

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Catalog No. T12434Cas No. 2070009-55-9

PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor with an IC50 of 16.1 nM, used as an anticancer agent.

PF-2771

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Catalog No. T12434Cas No. 2070009-55-9

PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor with an IC50 of 16.1 nM, used as an anticancer agent.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
100 mg	$1,490	6-8 weeks	6-8 weeks

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

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	PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor with an IC50 of 16.1 nM, used as an anticancer agent.
Targets&IC50	CENP-E:16.1 nM
In vitro	PF-2771 is a powerful and selective inhibitor of CENP-E, demonstrating significant inhibition of CENP-E motor activity at an IC50 of 16.1 nM, without affecting ATPase activities of similar kinesins (showing 0% inhibition of Eg5/KSP, chromokinesin, and MCAK at both 1 or 10 μM concentrations). It also displays negligible inhibitory effects on 74 protein kinases (less than 23% inhibition at 1 μM and less than 40% at 10 μM). Notably, PF-2771 is cytotoxic exclusively to basal-like breast cancer cells, with EC50 values below 0.1 μM, while it has no cytotoxic effects on normal and premalignant cell lines (EC50 > 5 μM). Furthermore, at 100 nM, PF-2771 induces a chromosomal congression defect in MDA-MB-468 cells.
In vivo	PF-2771 (100 mg/kg, daily i.p.) effectively inhibits CENP-E motor function, resulting in tumor regression in SCID mice with AA1077 mammary tumors [1].

Chemical Properties

Molecular Weight	554.08
Formula	C₂₉H₃₆ClN₅O₄
Cas No.	2070009-55-9
Smiles	CC(C)Oc1ccc(cc1Cl)C(=O)N[C@H](CNC(=O)CN(C)C)Cc1ccc(cc1)-c1cn(C)c(n1)C(C)=O
Relative Density.	1.22 g/cm3 (Predicted)

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: 32 mg/mL (57.75 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (3.61 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	1.8048 mL	9.0240 mL	18.0479 mL	90.2397 mL
5 mM	0.3610 mL	1.8048 mL	3.6096 mL	18.0479 mL
10 mM	0.1805 mL	0.9024 mL	1.8048 mL	9.0240 mL
20 mM	0.0902 mL	0.4512 mL	0.9024 mL	4.5120 mL
50 mM	0.0361 mL	0.1805 mL	0.3610 mL	1.8048 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