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CAS No. : 1538604-68-0
MCE 国际站:BLU9931
产品活性:BLU9931 是一种有效的,高度选择性的,不可逆的成纤维细胞生长因子受体 4 (FGFR4) 抑制剂,其 IC50 值为 3 nM,Kd 值为 6 nM。BLU9931 具有显着的抗肿瘤活性。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:FGFR
In Vitro: BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, with EC50s of 0.07 μM, 0.11 μM and 0.02 μM for Hep 3B, HuH7 and JHH7 cells, respectively.
BLU9931 (0.3-300 nM; 1 hour; MDA-MB-453 and Hep 3B cells) treatment demonstrates potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 cells. BLU9931 shows dose-dependent inhibition of the signaling cascade downstream of FGFR4. BLU9931 exhibits potent inhibition of phosphorylation of the FGFR4 pathway components in Hep 3B cells. BLU9931 treatment leads to induction of caspase-3/7 activity, indicative of induction of apoptosis that results in inhibition of signaling downstream of FGFR4.
BLU9931 (100 nM; 0 -24 hours; Hep 3B cells) treatment increases CYP7A1 mRNA expression and the expression of the proliferative marker EGR1 is inhibited.
In Vivo: BLU9931 (10-100 mg/kg; oral administration; twice every day; for 21 days; mice) treatment demonstrates antitumor activity in HCC xenograft models.
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 | Chemical Probe 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 | 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 | MAX-40279 hemifumarate | Pazopanib-13C,d3 hydrochloride
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货号: HY-12823
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