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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 Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $198 | 7-10 days | |
5 mg | $399 | 7-10 days | |
1 mL x 10 mM (in DMSO) | $546 | 7-10 days |
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. |
Molecular Weight | 596.74 |
Formula | C33H36N6O3S |
Cas No. | 1133432-49-1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 32 mg/mL (53.62 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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