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CSN5i-3

Name: CSN5i-3
Brand: TargetMol
SKU: T10895
Price: 378 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T10895Cas No. 2375740-98-8

CSN5i-3 is a potent, selective, and orally available inhibitor of the proteolytic subunit of the CSN complex, CSN5. It inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM. CSN5i-3 has a killing effect on a variety of cancer cells and can be used as an anticancer drug. [2]

CSN5i-3

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Purity: 99.73%

Catalog No. T10895Cas No. 2375740-98-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$378	In Stock	In Stock
5 mg	$813	In Stock	In Stock
10 mg	$1,230	In Stock	In Stock
25 mg	$1,830	In Stock	In Stock
50 mg	$2,470	In Stock	In Stock
100 mg	$3,330	-	In Stock
1 mL x 10 mM (in DMSO)	$886	In Stock	In Stock

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Batch Information

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Purity:99.73%

ee:100%

Appearance:Solid

Color:White to Yellow

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COA LCMS CSFC FNMR HNMR ORP

Product Introduction

Bioactivity

Description	CSN5i-3 is a potent, selective, and orally available inhibitor of the proteolytic subunit of the CSN complex, CSN5. It inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM. CSN5i-3 has a killing effect on a variety of cancer cells and can be used as an anticancer drug. [2]
Targets&IC50	CSN5:5.8 nM, CSN:∼5.4 nM
In vitro	METHODS: BV2 microglial cell line cells were pretreated with 1 or 4 μM CSN5i-3 for 2-4 hours to test whether treatment of BV2 cells with CSN5i-3 would result in an increase in NEDDylated CUL1 levels. RESULTS Treatment of BV2 cells with CSN5i-3 for 4 hours under basal conditions required only normal "cell culture stress" to result in an increase in NEDDylated CUL1, accompanied by a decrease in unmodified CUL1 levels, and CSN5i-3-treated BV2 cells showed a shift from a de-NEDDylated cullin band to a NEDD8-CUL1 band. [1]
In vivo	METHODS: Subcutaneous SU-DHL-1 xenografts were implanted in SCID-bg mice and CSN5i-3 (50, 100 mg/kg, oral, once daily) was used to observe the growth of CSN5i-3 human xenograft models in vivo. RESULTS CSN5i-3 inhibited tumor growth in the mouse model of human xenografts. [2]

Chemical Properties

Molecular Weight	505.56
Formula	C₂₈H₂₉F₂N₅O₂
Cas No.	2375740-98-8
Smiles	CC(C)n1nc(cc1C(=O)Nc1ccc([C@H]2[C@@H](O)CCCc3cncn23)c(c1)-c1ccccc1)C(F)F
Relative Density.	1.35 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: 247.5 mg/mL (489.56 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.89 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	1.9780 mL	9.8900 mL	19.7800 mL	98.9002 mL
5 mM	0.3956 mL	1.9780 mL	3.9560 mL	19.7800 mL
10 mM	0.1978 mL	0.9890 mL	1.9780 mL	9.8900 mL
20 mM	0.0989 mL	0.4945 mL	0.9890 mL	4.9450 mL
50 mM	0.0396 mL	0.1978 mL	0.3956 mL	1.9780 mL
100 mM	0.0198 mL	0.0989 mL	0.1978 mL	0.9890 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