Fostamatinib (R788) disodium hexahydrate is the oral prodrug of the active compound R406^[1]. R406 is an orally available and competitiveSyk/FLT3inhibitor with aK_iof 30 nM and anIC₅₀of 41 nM^[2]. R406 also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM)^[3].

Syk, FLT3^[2]

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: AUC_{0-16 hrs}= 10618 ng*h/mL and 30650 ng*h/mL respectively; C_max=2600 ng/mL and 6500 ng/mL respectively (observed at 1 hour); t_1/2=4.2 hours. The prodrug was not detected in plasma suggesting R788 is completely converted to R406^[1].

732.51

Solid

C₂₃H₃₆FN₆Na₂O₁₅P

914295-16-2

福他替尼二钠盐六水合物

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

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

DMSO : 25 mg/mL(34.13 mM;Need ultrasonic)

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

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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