| 产品描述： | Fostamatinib Disodium (R788 Disodium) is the oral prodrug of the active compound R406. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) |
| 靶点： |
Syk, FLT3;FLT;Syk |
| 体内研究： |
Fostamatinib (R788) is highly bioavailable, and rapidly absorbed in Louvain rats. R406 following a single oral dose of R788 10 mg/kg or 20 mg/kg: AUC0-16 hrs= 10618 ng*h/mL and 30650 ng*h/mL respectively; Cmax=2600 ng/mL and 6500 ng/mL respectively (observed at 1 hour); t1/2=4.2 hours. The prodrug was not detected in plasma suggesting R788 is completely converted to R406 |
| 参考文献： |
1. Stephen P McAdoo, et al. Fostamatinib Disodium. Drugs Future. 2011;36(4):273. 2. Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. 3. Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317(2):571-8. |
| 溶解性： |
DMSO : 20.83 mg/mL (33.36 mM; ultrasonic and warming and heat to 60°C) H2O : ≥ 1 mg/mL (1.60 mM) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.601 ml |
8.007 ml |
16.015 ml |
| 5 mM |
0.32 ml |
1.601 ml |
3.203 ml |
| 10 mM |
0.16 ml |
0.801 ml |
1.601 ml |
| 50 mM |
0.032 ml |
0.16 ml |
0.32 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