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GSK3186899

Name: GSK3186899
Brand: TargetMol
SKU: T15438
Price: 148 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15438Cas No. 1972617-87-0

Alias DDD-853651, 3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamide

GSK3186899 is an inhibitor of Cdc2-related kinase 12 with an EC50 of 1.4 μM for L. donovani.

GSK3186899

😃Good

Purity: 99.61%

Catalog No. T15438Alias DDD-853651, 3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamideCas No. 1972617-87-0

GSK3186899 is an inhibitor of Cdc2-related kinase 12 with an EC50 of 1.4 μM for L. donovani.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$148	In Stock	In Stock
5 mg	$323	In Stock	In Stock
10 mg	$491	In Stock	In Stock
25 mg	$833	In Stock	In Stock
50 mg	$1,110	-	In Stock
100 mg	$1,450	-	In Stock
200 mg	$1,960	-	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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Batch Information

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Purity:99.61%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	GSK3186899 is an inhibitor of Cdc2-related kinase 12 with an EC50 of 1.4 μM for L. donovani.
In vitro	GSK3186899 is active in cidal axenic amastigote assay with an EC50 value of 0.1 μM. GSK3186899 shows good selectivity against mammalian THP-1 host cells (EC50 value > 50 μM). GSK3186899 exhibits a less than 10-fold variation in potency against a panel of Leishmania-derived lines. GSK3186899 is more active using human peripheral blood mononuclear cells as the host cells[1].
In vivo	In the mouse model of infection, GSK3186899 (25 mg/kg; orally) reduces parasite levels by 99%. The efficacy of treatment is dependent on dose, frequency, and duration (10 days better than 5). There are no notable adverse effects in a rat seven-day repeat-dose oral toxicity study with respect to clinical chemistry and histopathology at all doses tested[1].
Synonyms	DDD-853651, 3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamide

Chemical Properties

Molecular Weight	491.53
Formula	C₁₉H₂₈F₃N₇O₃S
Cas No.	1972617-87-0
Smiles	C[C@H]1CN(CCO1)c1n[nH]c2nc(N[C@H]3CC[C@@H](CC3)NS(=O)(=O)CCC(F)(F)F)ncc12
Relative Density.	no data available

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: 200 mg/mL (406.89 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.17 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	2.0345 mL	10.1723 mL	20.3446 mL	101.7232 mL
5 mM	0.4069 mL	2.0345 mL	4.0689 mL	20.3446 mL
10 mM	0.2034 mL	1.0172 mL	2.0345 mL	10.1723 mL
20 mM	0.1017 mL	0.5086 mL	1.0172 mL	5.0862 mL
50 mM	0.0407 mL	0.2034 mL	0.4069 mL	2.0345 mL
100 mM	0.0203 mL	0.1017 mL	0.2034 mL	1.0172 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