GDC-0834 Racemate是GDC-0834的外消旋体形式。

GDC-0834 Racemate is the racemate form of GDC-0834, which is a potent and selective BTK inhibitor with in vitro IC50s of 5.9 and 6.4 nM in biochemical and cellular assays, respectively. IC50 value: 5.9 nM/6.4 nM(biochemical/cellular assay) [1] Target: BTK in vitro: GDC-0834 inhibited BTK with an in vitro IC(50) of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC(50) of 1.1 and 5.6 μM in mouse and rat, respectively [1]. in vivo: Administration of GDC-0834 (30-100 mg/kg) in a rat collagen-induced arthritis (CIA) model resulted in a dose-dependent decrease of ankle swelling and reduction of morphologic pathology [1]. GDC-0834 exhibited low clearance in PXB chimeric mice with humanized liver. Uncertainty in human pharmacokinetic prediction and high interest in a BTK inhibitor for clinical evaluation prompted an investigational new

Solid

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Liu L, et al. Antiarthritis effect of a novel Brutons tyrosine kinase (BTK) inhibitor in rat collagen-induced arthritis and mechanism-based pharmacokinetic/pharmacodynamic modeling: relationships between inhibition of BTK phosphorylation and efficacy. J
[2]. Liu L, et al. Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Brutons tyrosine kinase inhibitor. Drug Metab Dispos. 2011 Oct;39(10):1840-9.

In Vitro: DMSO : 100 mg/mL (167.58 mM; Need ultrasonic)配制储备液