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。

Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC 50 of 1.9 nM. Roblitinib has antitumor activity.

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FGFR4 1.9 nM (IC50) FGFR1 >10 μM (IC

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).
has not independently confirmed the accuracy of these methods. They are for reference only.

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Nicole Buschmann, et al. Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors. WO2015059668A1.
[2]. Robin A Fairhurst, et al. Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. J Med Chem. 2020 Nov 12;63(21):12542-12573.

In Vitro: DMSO : 5.2 mg/mL (10.27 mM; Need ultrasonic)配制储备液