GDC-0834_product_DataBase

Bioactivity

GDC-0834 is a potent and selective BTK inhibitor. 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.

Target

IC50: 5.9 nM (BTK)

Invitro

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.)[1]. 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[2].

In Vivo

The treatment of BALB/c mice with GDC-0834 results in dose-dependent inhibition of pBTK-Tyr223. Animals dosed with 150 or 100 mg/kg GDC-0834 for 2 h show complete inhibition of pBTK-Tyr223 levels in blood, with a mean inhibition of 97 and 96%, respectively. In the rat CIA study, GDC-0834 inhibits pBTK-Tyr223 in rat blood in a dose-dependent manner. The IC50 estimate of pBTK-Tyr223 inhibition in rats is determined to be 5.6±1.6 μM with m of 0.51±0.087 (mean±S.E.)[1].

Name

GDC-0834

CAS

1133432-49-1

Formula

C33H36N6O3S

Molar Mass

596.74

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Liu L, et al. Antiarthritis effect of a novel Bruton's 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]. Sodhi JK, et al. A novel reaction mediated by human aldehyde oxidase: amide hydrolysis of GDC-0834. Drug Metab Dispos. 2015 Jun;43(6):908-15

PeptideDB

GDC-0834

CAS: 1133432-49-1 F: C33H36N6O3S W: 596.74