Fostamatinib-d9 (R788-d9) is the deuterium labeled Fostamatinib. Fostamatinib (R788) is the oral prodrug of the active compound R406[1]. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM[2]. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[3].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
589.51
Formula
C23H17D9FN6O9P
CAS 号
1260832-60-7
中文名称
福他替尼 d9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Stephen P McAdoo, et al. Fostamatinib Disodium. Drugs Future. 2011;36(4):273.
[3]. 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.
[4]. 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.
Fostamatinib (R788) is the oral prodrug of the active compound R406[1]. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM[2]. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[3].
IC50 & Target
Syk, FLT3[2]
体内研究 (In Vivo)
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[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
580.46
Formula
C23H26FN6O9P
CAS 号
901119-35-5
中文名称
福他替尼
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 62.5 mg/mL (107.67 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
Fostamatinib Disodium (R788 Disodium) is the oral prodrug of the active compound R406[1]. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM[2]. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[3].
IC50 & Target
Syk, FLT3[2]
体内研究 (In Vivo)
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[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
624.42
Formula
C23H24FN6Na2O9P
CAS 号
1025687-58-4
中文名称
福他替尼二钠盐
运输条件
Room temperature in continental US; may vary elsewhere.
Fostamatinib disodium hexahydrate Chemical Structure
CAS No. : 914295-16-2
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生物活性
Fostamatinib (R788) disodium hexahydrate is the oral prodrug of the active compound R406[1]. R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM[2]. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[3].
IC50 & Target
Syk, FLT3[2]
体内研究 (In Vivo)
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[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
732.51
Formula
C23H36FN6Na2O15P
CAS 号
914295-16-2
中文名称
福他替尼二钠盐六水合物
运输条件
Room temperature in continental US; may vary elsewhere.