S80029
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- 公司名稱 上海源葉生物科技有限公司
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- 廠商性質(zhì) 生產(chǎn)廠家
- 更新時間 2024/7/3 18:55:13
- 訪問次數(shù) 124
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- 產(chǎn)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)
- 靶點(diǎn)： Syk, FLT3
- 體內(nèi)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
- 參考文獻(xiàn)：
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.
- 溶解度： DMSO : 20.83 mg/mL (33.36 mM; ultrasonic and warming and heat to 60°C) H2O : ≥ 1 mg/mL (1.60 mM)
- 保存條件： -20℃
- 配置溶液濃度參考：
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
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