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GDC-0834

GDC-0834
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GDC-0834

Catalog No. T11379Cas No. 1133432-49-1
GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively. GDC-0834 is a potent and selective BTK inhib
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Pack SizePriceAvailabilityQuantity
2 mg$1987-10 days
5 mg$3997-10 days
1 mL x 10 mM (in DMSO)$5467-10 days
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Product Introduction

Bioactivity
Description
GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively. GDC-0834 is a potent and selective BTK inhib
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
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 32 mg/mL (53.62 mM)
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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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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