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GDC-0834

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Catalog No. T11379Cas No. 1133432-49-1

GDC-0834 is a potent and selective BTK inhibit that inhibits BTK with an in vitro IC50 of 5.9 nM (biochemical assays) and 6.4 nM (cellular assays), and with an in vivo IC50 of 1.1 μM (mouse) and 5.6 μM (rat).

GDC-0834

GDC-0834

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Catalog No. T11379Cas No. 1133432-49-1
GDC-0834 is a potent and selective BTK inhibit that inhibits BTK with an in vitro IC50 of 5.9 nM (biochemical assays) and 6.4 nM (cellular assays), and with an in vivo IC50 of 1.1 μM (mouse) and 5.6 μM (rat).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$1987-10 days7-10 days
5 mg$3997-10 days7-10 days
1 mL x 10 mM (in DMSO)$5467-10 days7-10 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
GDC-0834 is a potent and selective BTK inhibit that inhibits BTK with an in vitro IC50 of 5.9 nM (biochemical assays) and 6.4 nM (cellular assays), and with an in vivo IC50 of 1.1 μM (mouse) and 5.6 μM (rat).
Targets&IC50
BTK:5.9 nM
In vitro
GDC-0834 is shown to be a potent reversible inhibitor of six known aldehyde oxidase (AO) substrates with IC50 values ranging from 0.86 to 1.87 μM.?GDC-0834 suppresses BTK kinase activity with an IC50 value of 5.9±1.1 nM with Hill slope value of ?0.84±0.07 (mean±S.E.).
In vivo
In a rat collagen-induced arthritis (CIA) study, GDC-0834 exhibits a dose-dependent inhibition of phosphorylated Bruton's tyrosine kinase (pBTK-Tyr223) in rat blood. The estimated half-maximal inhibitory concentration (IC50) for pBTK-Tyr223 inhibition in rats is 5.6±1.6 μM, demonstrating a moderate potency with a mean (m) value of 0.51±0.087. Furthermore, treatment with GDC-0834 in BALB/c mice demonstrates dose-dependent suppression of pBTK-Tyr223, with dosages of 150 or 100 mg/kg achieving nearly complete inhibition (97% and 96%, respectively) of pBTK-Tyr223 levels in the blood after 2 hours.
Chemical Properties
Molecular Weight596.74
FormulaC33H36N6O3S
Cas No.1133432-49-1
SmilesCN1CCN(C)C(=O)[C@H]1c1ccc(Nc2nc(cn(C)c2=O)-c2cccc(NC(=O)c3cc4CCCCc4s3)c2C)cc1
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: 32 mg/mL (53.62 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6758 mL8.3789 mL16.7577 mL83.7886 mL
5 mM0.3352 mL1.6758 mL3.3515 mL16.7577 mL
10 mM0.1676 mL0.8379 mL1.6758 mL8.3789 mL
20 mM0.0838 mL0.4189 mL0.8379 mL4.1894 mL
50 mM0.0335 mL0.1676 mL0.3352 mL1.6758 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:
mg/kg
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μL
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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