|(R)-N-(3-(6-((4-(1,4-二甲基-3-氧代哌嗪-2-基)苯基)氨基)-4-甲基-5-氧代-4,5-二氢吡嗪-2-基)-2-甲基苯基)-4,5,6,7-四氢苯并[b]噻吩-2-甲酰胺|CsnPharm

CAS No.: 1133432-49-1

GDC-0834 Catalog No. CSN17490

Synonyms: Gdc-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.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6758 mL
- 8.3788 mL
- 16.7576 mL
- 5 mM
- 0.3352 mL
- 1.6758 mL
- 3.3515 mL
- 10 mM
- 0.1676 mL
- 0.8379 mL
- 1.6758 mL

技术信息

CAS号

1133432-49-1

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H36N6O3S

运输

蓝冰

分子量

596.74

别名

Gdc-0834

溶解度

DMSO	32.0 mg/mL (53.6 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

GDC-0834 Catalog No. CSN17490

靶点选择性

请登录您的专属账户

确认信息