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Darovasertib

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

🥰Excellent

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

🥰Excellent

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	Availability
1 mg	$48	In Stock
5 mg	$138	In Stock
10 mg	$198	In Stock
25 mg	$369	In Stock
50 mg	$549	In Stock
100 mg	$789	In Stock
200 mg	$1,080	In Stock
1 mL x 10 mM (in DMSO)	$152	In Stock

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Purity:99.89%

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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	GSK-3β:3.1 μM, PKCθ:0.4 nM , PKCα:1.9 nM
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: 100 mg/mL (211.65 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
50 mM	0.0423 mL	0.2117 mL	0.4233 mL	2.1165 mL
100 mM	0.0212 mL	0.1058 mL	0.2117 mL	1.0583 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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

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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