化合物BLU554 T3456

Product Introduction
Bioactivity


英文名: Fisogatinib

描述: Fisogatinib (BLU-554) 是高效的、选择性的、口服具有活力的 FGFR4 抑制剂(IC50:5 nM)。它在依赖FGFR4信号传导的肝细胞癌模型中具有显著的抗肿瘤活性。

激酶实验: The Ki value and mode of inhibition of LY2801653 for the MET kinase activity are determined using a radiometric filter-binding assay. Reactions are carried out in 96-well plates in Enzyme dilution buffer (EDB) compose of 50 mM Tris HCl pH 7.5, 2 mM DTT, 0.005% Triton X-100, 10 mM MgCl2, and 250 ?M EDTA. Serially diluted LY2801653 (final concentration 250 to 0 nM) are followed by the addition of a series of 8 concentrations of 33P-γ-ATP (final concentration 400 to 10 μM ATP), and 5 nM enzyme (final concentration). After a 2-hour incubation, PolyGluTyr synthetic protein substrate (final 150 μg/mL) is added to initiate the 30-minute kinase reaction. Reactions are quenched with 10% H3PO4, transfer to a pre-wetted Multiscreen anionic phosphocellulose 96-well filter plate, and washed; radioactivity is measured with a scintillation counter. The experimental data are fit to a global mix model inhibition equation using GraphPad Prism softwar to generate an alpha value to determine the modality of inhibition and to calculate the Ki value for LY2801653[1].

体外活性: BLU-554 exploits a unique interaction with FGFR4 to confer potency and selectivity

体内活性: BLU-554 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 2 mg/mL (3.97 mM)
DMSO : 93 mg/mL (184.8 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: inhibit | FGFR | Fisogatinib | Fibroblast growth factor receptor | Inhibitor

相关产品: Dovitinib lactate hydrate | FGFR2-IN-3 | Masitinib mesylate | FGFR3-IN-7 | ENMD-2076 | BLU9931 | S6K2-IN-1 | SSR128129E | SKLB 610 | PRN1371

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Osteogenesis Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Highly Selective Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途