Fostamatinib disodium hexahydrate(Synonyms: 福他替尼二钠盐六水合物; R788 disodium hexahydrate)

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Fostamatinib disodium hexahydrate (Synonyms: 福他替尼二钠盐六水合物; R788 disodium hexahydrate) 纯度: 98.94%

Fostamatinib (R788) disodium hexahydrate 是 R406 的口服前药。R406 是一种有效的，具有口服活性的，ATP 竞争性的 Syk/FLT3 抑制剂，Ki 为 30 nM，IC50 为 41 nM。R406 还抑制 Lyn (IC50=63 nM) 和 Lck (IC50=37 nM).

Fostamatinib disodium hexahydrate(Synonyms: 福他替尼二钠盐六水合物; R788 disodium hexahydrate)

Fostamatinib disodium hexahydrate Chemical Structure

CAS No. : 914295-16-2

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10 mM * 1 mL in DMSO ￥1612 In-stock
5 mg ￥1000 In-stock
10 mg ￥1600 In-stock
50 mg ￥4500 In-stock
100 mg ￥7500 In-stock
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Fostamatinib disodium hexahydrate 相关产品

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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.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 31.81 mg/mL (43.43 mM; Need ultrasonic)

H2O : 2 mg/mL (2.73 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3652 mL 6.8258 mL 13.6517 mL
5 mM 0.2730 mL 1.3652 mL 2.7303 mL
10 mM 0.1365 mL 0.6826 mL 1.3652 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： Cremophor EL

    Solubility: 10 mg/mL (13.65 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 0.5% CMC-Na/saline water

    Solubility: 8.33 mg/mL (11.37 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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