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蛋白质酪氨酸激酶
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GDC-0834 {[allProObj[0].p_purity_real_show]}

货号：A190491

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.

GDC-0834 化学结构 CAS号：1133432-49-1
GDC-0834 化学结构
CAS号：1133432-49-1
GDC-0834 3D分子结构
CAS号：1133432-49-1
GDC-0834 化学结构 CAS号：1133432-49-1
GDC-0834 3D分子结构 CAS号：1133432-49-1
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GDC-0834 纯度/质量文件 产品仅供科研

货号：A190491 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 BTK ↓ 其他靶点 纯度
CGI-1746 +++

BTK, IC50: 1.9 nM

 		98%
Spebrutinib ++++

BTK, IC50: <0.5 nM

 		98+%
Acalabrutinib ++

BTK, IC50: 3nM

 		98%
CNX-774 +++

BTK, IC50: <1 nM

 		99%+
Ibrutinib ++++

BTK, IC50: 0.5 nM

 		98%
ONO-4059 analog +

BTK, IC50: 23.9 nM

 		98%
RN486 ++

BTK, IC50: 4 nM

 		99%+
(Z)-LFM-A13 +

BTK, Ki: 1.4 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

GDC-0834 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].

GDC-0834 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

GDC-0834 实验方案

计算器
存储液制备 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

GDC-0834 技术信息

CAS号1133432-49-1
分子式C33H36N6O3S
分子量 596.742
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

Tags: GDC-0834 | 1133432-49-1 | GDC0834 | GDC 0834 | Btk Inhibitor | Protein Tyrosine Kinase/RTK | Btk | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | GDC-0834 纯度/质量文件 | GDC-0834 亚型比较 | GDC-0834 生物活性 | GDC-0834 参考文献 | GDC-0834 实验方案 | GDC-0834 技术信息

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