| 产品描述： | Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity |
| 靶点： |
IC50: 0.68 nM (Bcr-AblT315I), 0.27 nM (Bcr-AblE255K) , 0.71 nM (Bcr-AblG250E) , 0.15 nM (Bcr-AblQ252H), 0.35 nM (Bcr-AblH396P), 0.29 nM (Bcr-AblM351T), 0.35 nM (Bcr-AblY253F), Bcr-AblF317L |
| 体内研究： |
Olverembatinib suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl WT.Olverembatinib (1-20 mg/kg; i.g.; daily; for 10 days) significantly increases the median survival of the mice bearing allografted Ba/F3 cells expressing Bcr-AblT315I. Olverembatinib exhibits a good oral bioavailability (rat 48.7%) and Cmax (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg). Olverembatinib exhibits terminal elimination half-lives (rat 5.6 h) due to high plasma clearance (rat 1.7 L/h/kg) following intravenous administration (rat 5 mg/kg) |
| 参考文献： |
1. Ren X, Pan X, Zhang Z, Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against |
| 溶解性： |
DMSO : 41.67 mg/mL (78.24 mM; ultrasonic and warming and heat to 60°C) |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.878 ml |
9.389 ml |
18.777 ml |
| 5 mM |
0.376 ml |
1.878 ml |
3.755 ml |
| 10 mM |
0.188 ml |
0.939 ml |
1.878 ml |
| 50 mM |
0.038 ml |
0.188 ml |
0.376 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京