GDC-0834

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Chemical Structure| 1133432-49-1 同义名 : -
CAS号 : 1133432-49-1
货号 : A190491
分子式 : C33H36N6O3S
纯度 : 98%+
分子量 : 596.742
MDL号 : MFCD22665722
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(50.27 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.68mL

0.34mL

0.17mL

8.38mL

1.68mL

0.84mL

16.76mL

3.35mL

1.68mL
参考文献

[1]Sodhi JK, Wong S, et al. A novel reaction mediated by human aldehyde oxidase: amide hydrolysis of GDC-0834. Drug Metab Dispos. 2015 Jun;43(6):908-15.

[2]Liu L, Di Paolo J,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 Pharmacol Exp Ther. 2011 Jul;338(1):154-63.

[3]Liu L, Di Paolo J, Barbosa J, Rong H, Reif K, Wong H. 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 Pharmacol Exp Ther. 2011;338(1):154-163. doi:10.1124/jpet.111.181545