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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 T1/2 of 1.4 hours, a CL of 28 mL/min•kg, and a Vss of 2.3 L/kg for Male mice (C57BL/6) .
Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T1/2 of 4.4 hours, a CL of 19 mL/min•kg, and a Vss of 3.9 L/kg for male SD rats.
相关产品:Covalent Screening Library Plus | Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Covalent Screening Library | Reprogramming Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Anti-Lung Cancer Compound Library | Angiogenesis-Related Compound Library | Targeted Diversity Library | Anti-Liver Cancer Compound Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | FGFR4-IN-12 | FGFR2-IN-2 | Multi-kinase-IN-2 | FGFR1 inhibitor-6 | FGFR4-IN-4 | FGFR3-IN-3 | FGFR-IN-7 | PP58 | FGFR4-IN-10 | Vosoritide acetate | ODM-203 | ENMD-2076 Tartrate | R1530 | Gunagratinib | Ponatinib hydrochloride | Nintedanib | Heparan Sulfate | CPL304110 | Futibatinib | Trafermin | PD173074 | FGFR-IN-2 | Lucitanib | Masitinib | Nintedanib-13C,d3 | Zoligratinib | BLU9931 | MAX-40279 hemifumarate | Pazopanib-13C,d3 hydrochloride
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