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2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide

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Catalog No. T22338Cas No. 1258292-64-6
Alias GDC046

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide (GDC046), a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile.

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide

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Purity: 98.77%
Catalog No. T22338Alias GDC046Cas No. 1258292-64-6
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide (GDC046), a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$43In StockIn Stock
5 mg$100In StockIn Stock
10 mg$165In StockIn Stock
25 mg$315In StockIn Stock
50 mg$489-In Stock
100 mg$759-In Stock
200 mg$987-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.77%
Appearance:Solid
Color:White
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Product Introduction

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide AI Summary
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide exhibits significant bioactivity as an inhibitor of Janus kinase (JAK) enzymes, particularly JAK1, JAK2, JAK3, and TYK2, with respective Ki values indicating high potency (e.g., 4.8 nM for TYK2 and 28.0 nM for JAK2). The compound has demonstrated selective inhibition of these kinases over others, such as CDK9, and inhibits STAT protein phosphorylation in cell-based assays. Its pharmacokinetic properties include moderate clearance rates, good oral bioavailability, high plasma protein binding, specific half-lives in rodents, and defined parameters for clearance, volume of distribution, solubility, and permeability. These characteristics suggest 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide's potential as a therapeutic agent targeting JAK-mediated pathways for various diseases. Moreover, the compound influences cell viability differently across cell types and shows varying effects on the thermal stability of protein domains, indicating a complex interaction profile with proteins..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide (GDC046), a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile.
Targets&IC50
JAK2:0.7 nM (Ki), JAK1:0.7 nM (Ki), TYK2:4.8 nM (Ki), JAK3:0.4 nM (Ki)
SynonymsGDC046
Chemical Properties
Molecular Weight350.2
FormulaC16H13Cl2N3O2
Cas No.1258292-64-6
SmilesClc1cccc(Cl)c1C(=O)Nc1ccnc(NC(=O)C2CC2)c1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 250 mg/mL (713.88 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.86 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
1mg5mg10mg50mg
1 mM2.8555 mL14.2776 mL28.5551 mL142.7756 mL
5 mM0.5711 mL2.8555 mL5.7110 mL28.5551 mL
10 mM0.2856 mL1.4278 mL2.8555 mL14.2776 mL
20 mM0.1428 mL0.7139 mL1.4278 mL7.1388 mL
50 mM0.0571 mL0.2856 mL0.5711 mL2.8555 mL
100 mM0.0286 mL0.1428 mL0.2856 mL1.4278 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

Keywords

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