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NSC305787 hydrochloride

Name: NSC305787 hydrochloride
Brand: TargetMol
SKU: T12263L
Price: 113 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T12263LCas No. 53868-26-1

Alias (Rac)-NSC305787 hydrochloride

NSC305787 hydrochloride ((Rac)-NSC305787 hydrochloride is a cell membrane permeable and selective and potent small molecule dual inhibitor of Cdc25 dual specificity phosphatase and EZR that displays antitumor activity in pancreatic cancer cells and inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.NSC 663284 inhibits NSD2 (IC50 of 170 nM) enzyme activity.

NSC305787 hydrochloride

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Purity: 99.07%

Catalog No. T12263LAlias (Rac)-NSC305787 hydrochlorideCas No. 53868-26-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$113	-	In Stock
2 mg	$166	5 days	5 days
5 mg	$277	5 days	5 days

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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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Batch Information

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Purity:99.07%

Appearance:Solid

Color:White

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COA MS HPLC

Product Introduction

Bioactivity

Description	NSC305787 hydrochloride ((Rac)-NSC305787 hydrochloride is a cell membrane permeable and selective and potent small molecule dual inhibitor of Cdc25 dual specificity phosphatase and EZR that displays antitumor activity in pancreatic cancer cells and inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.NSC 663284 inhibits NSD2 (IC50 of 170 nM) enzyme activity.
Targets&IC50	Radixin:55 μM, PKCΙ:172.4 μM (Kd), MBP:58.9 μM, Ezrin:5.85 μM (Kd), Ezrin:8.3 μM, Moesin:9.4 μM
In vitro	NSC305787 hydrochloride, an inhibitor of ezrin, exhibits a Kd of 5.85 μM and demonstrates antitumor activity. With IC50 values of 8.3, 9.4, 55, and 58.9 μM, NSC305787 hydrochloride inhibits PKCΙ phosphorylation of Ezrin, Moesin, Radixin, and MBP, respectively. Binding to PKCΙ with a Kd value of 172.4 μM, NSC305787 hydrochloride primarily inhibits ezrin T567 phosphorylation through its binding to ezrin, not via the inhibition of PKCΙ kinase activity. In the context of K7M2 osteosarcoma (OS) cells, NSC305787 hydrochloride (1, 10 μM) displays inhibitory activity against ezrin-mediated invasion. Furthermore, at a concentration of 10 μM, NSC305787 hydrochloride diminishes cell motility phenotypes in zebrafish and hinders OS metastatic growth in lung organ culture[2].
In vivo	In a mouse model,NSC305787 hydrochloride (i.p., 0.240 mg/kg/day) effectively suppresses ezrin-dependent osteosarcoma metastatic growth in the lung[1]. Additionally, in a transgenic mouse model of osteosarcoma (Osx-Cre+p53fl/flpRBfl/fl), NSC305787 hydrochloride (i.p., 240 μg/kg) exhibits a remarkable inhibition of pulmonary metastasis. Furthermore, it demonstrates a more favorable pharmacokinetic profile compared to NSC668394 in the same mouse model[1].
Synonyms	(Rac)-NSC305787 hydrochloride

Chemical Properties

Molecular Weight	481.89
Formula	C₂₅H₃₁Cl₃N₂O
Cas No.	53868-26-1
Smiles	Cl.OC(C1CCCCN1)c1cc(nc2c(Cl)cc(Cl)cc12)C12CC3CC(CC(C3)C1)C2
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 5 mg/mL (10.38 mM), Sonication is recommended.

H2O: <0.1 mg/mL (Insoluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.08 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	2.0752 mL	10.3758 mL	20.7516 mL	103.7581 mL
5 mM	0.4150 mL	2.0752 mL	4.1503 mL	20.7516 mL
10 mM	0.2075 mL	1.0376 mL	2.0752 mL	10.3758 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