CAS:1133432-49-1GDC-0834

GDC-0834 is a potent and selective BTK inhibitor with in vitro IC50s of 5.9 and 6.4 nM in biochemical and cellular assays, respectively.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1133432-49-1

储存条件

分子式

C33H36N6O3S

运输

蓝冰

分子量

596.74

别名

溶解度

DMSO	32.0 mg/mL (53.6 mM)

动物实验配方

生物活性

描述Bruton's tyrosine kinase (BTK) is a non-receptor tyrosine kinase that can be activated by phosphorylation, leading to the activation of NF-κB- and nuclear factor of activated T cell-dependent pathways. GDC-0834 is a BTK inhibitor with IC50 values of 5.9±1.1 and 6.4±1.6 nM in biochemical and cellular assays, respectively. The in vivo IC50 values of GDC-0834 are 1.1 and 5.6 μM in mouse and rat, respectively. Treatment of BALB/c mice with 100 or 150mg/kg GDC-0834 for 2 h dose-dependently inhibited pBTK-Tyr223 in the blood (96% and 97% inhibition, respectively). GDC-0834 at a dosage of 30 or 100 mg/kg significantly reduced the area under the ankle diameter-time curve in rats when administered once per day or twice daily. Compared to vehicle-treated controls, the ankle histopathology parameters in rats treated with 100 mg/kg GDC-0834 were significantly reduced when administered twice daily (78% reduction), once daily (78% reduction), or every other day (38% reduction)^[3].