GDC-0834
规格
| Cas Number | 1133432-49-1 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 50mg 或 10mg 或 5mg 或 2mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : ≥ 32 mg/mL (53.62 mM) |
| 过滤标签 | Btk,Protein Tyrosine Kinase/RTK |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | GDC-0834 是一种强效的选择性 BTK 抑制剂。GDC-0834 抑制 BTK 的体外 IC 50 在生化和细胞试验中分别为 5.9 和 6.4 nM，在小鼠和大鼠体内的 IC 50 分别为 1.1 和 5.6 μM。 |
| 英文描述 |
GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC 50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC 50 of 1.1 and 5.6 μM in mouse and rat, respectively. In Vitro GDC-0834 suppresses BTK kinase activity with an IC 50 value of 5.9±1.1 nM with Hill slope value of −0.84±0.07 (mean±S.E.). GDC-0834 is shown to be a potent reversible inhibitor of six known aldehyde oxidase (AO) substrates with IC 50 values ranging from 0.86 to 1.87 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 IC 50 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.) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 5.9 nM (BTK) |