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Fostamatinib Disodium

CAS No. : 1025687-58-4

MCE 站：Fostamatinib Disodium

产品活性：Fostamatinib Disodium (R788 Disodium) 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，K_i 为 30 nM，IC₅₀ 为 41 nM。R406 还抑制 Lyn (IC₅₀=63 nM) 和 Lck (IC₅₀=37 nM).

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Syk  |  FLT3

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: 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.

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