Roblitinib

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Roblitinib

CAS No. : 1708971-55-4

MCE 国际站：Roblitinib

产品活性：Roblitinib (FGF-401) 是一种口服有效的，高选择性的 FGFR4 抑制剂，IC₅₀ 为 1.9 nM。Roblitinib 有抗癌活性。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FGFR

In Vitro: Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor (IC₅₀= 1.9 nM).
Roblitinib shows no activity FGFR1, FGFR2, FGFR3, rat FGFR4, C552A FGFR4 (all IC₅₀>10 uM).
Roblitinib inhibits HUH7 (IC₅₀=12 nM), Hep3B (IC₅₀=9 nM), JHH7 (IC₅₀=9 nM), HEPG2 (IC₅₀>10 uM), JHH (IC₅₀>10 uM).

In Vivo: Roblitinib (gavage; 10-100 mg/kg; b.i.d.; for 10 days) with the 30 mg/kg has the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model.
Roblitinib causes blood concentrations dropped below the IC90 threshold level within 8 h of dosing, and controlles tumor growth to the level of stasis at the lowest dose of 10 mg/kg for 6 days.
Roblitinib (iv at 1 mg/kg; po at 3 mg/kg) has a T_1/2 of 1.4 hours, a CL of 28 mL/min•kg, and a V_ss of 2.3 L/kg for Male mice (C57BL/6) .
Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T_1/2 of 4.4 hours, a CL of 19 mL/min•kg, and a V_ss of 3.9 L/kg for male SD rats.

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