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CAS No. : 1628793-01-0
MCE 国际站:FGFR4-IN-5
产品活性:FGFR4-IN-5 是一种有效的选择性共价 FGFR4 抑制剂,IC50 为 6.5 nM。FGFR4-IN-5 具有较强的抗肿瘤活性,可用于肝癌研究。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:FGFR
In Vivo: FGFR4-IN-5 (oral gavage; 10 mg/kg; single dose) reveals a high Cmax, low clearance, the Cmax values are 423 ng/ml, 588 ng/ml, and 2820 ng/ml in mice, rat and cynamolgus monkey, respectively. And the oral bioavailability are 20, 12, and 27% in mouse, rat, and cyno, respectively.FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) exhibits strong antitumor activity in an orthotopic Hep3B HTX model.FGFR4-IN-5 (oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days) results in dose-dependent growth inhibition of resistant tumors. Tumor regression is observed at 30 and 100 mg/kg, with %ΔT/ΔC of 67% and 70%, respectively. However, treatment with sorafenib at 100 mg/kg once daily does not provide any benefit in vivo.
相关产品:Covalent Screening Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Covalent Screening Library | Reprogramming Compound Library | Orally Active Compound Library | Anti-Lung Cancer Compound Library | Angiogenesis-Related Compound 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 | Roblitinib | PD173074 | FGFR-IN-2 | Lucitanib | Masitinib | Nintedanib-13C,d3 | Zoligratinib | BLU9931 | MAX-40279 hemifumarate | Pazopanib-13C,d3 hydrochloride
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-131704
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