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Darovasertib

Name: Darovasertib
Brand: TargetMol
SKU: T5600
Price: 48 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5600Cas No. 1874276-76-2

Alias LXS196

Darovasertib (LXS196) is a potent, selective, and orally active protein kinase C (PKC) inhibitor with IC50 values of 1.9 nM for PKCα, 0.4 nM for PKCθ, and 3.1 μM for GSK3β.

Darovasertib

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Purity: 99.89%

Catalog No. T5600Alias LXS196Cas No. 1874276-76-2

Darovasertib (LXS196) is a potent, selective, and orally active protein kinase C (PKC) inhibitor with IC50 values of 1.9 nM for PKCα, 0.4 nM for PKCθ, and 3.1 μM for GSK3β.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
5 mg	$138	In Stock	In Stock
10 mg	$198	In Stock	In Stock
25 mg	$369	In Stock	In Stock
50 mg	$529	In Stock	In Stock
100 mg	$778	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$145	In Stock	In Stock

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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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Purity:99.89%

Appearance:Solid

Color:White to Yellow

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	Darovasertib (LXS196) is a potent, selective, and orally active protein kinase C (PKC) inhibitor with IC50 values of 1.9 nM for PKCα, 0.4 nM for PKCθ, and 3.1 μM for GSK3β.
Targets&IC50	PKCθ:0.4 nM , PKCα:1.9 nM , GSK-3β:3.1 μM
In vitro	An orally available protein kinase C (PKC) inhibitor with potential immunosuppressive and antineoplastic activities. Upon oral administration, protein kinase C inhibitor Darovasertib binds to and inhibits PKC, which prevents the activation of PKC-mediated signaling pathways. This may lead to the induction of cell cycle arrest and apoptosis in susceptible tumor cells. PKC, a serine/threonine protein kinase overexpressed in certain types of cancer cells, is involved in tumor cell differentiation, proliferation, invasion and survival.
Synonyms	LXS196

Chemical Properties

Molecular Weight	472.47
Formula	C₂₂H₂₃F₃N₈O
Cas No.	1874276-76-2
Smiles	CC1(N)CCN(CC1)c1cccnc1NC(=O)c1nc(cnc1N)-c1ncccc1C(F)(F)F
Relative Density.	1.387 g/cm3 (Predicted)

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: 16.67 mg/mL (35.28 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.47 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	2.1165 mL	10.5827 mL	21.1654 mL	105.8268 mL
5 mM	0.4233 mL	2.1165 mL	4.2331 mL	21.1654 mL
10 mM	0.2117 mL	1.0583 mL	2.1165 mL	10.5827 mL
20 mM	0.1058 mL	0.5291 mL	1.0583 mL	5.2913 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