化合物FIIN-1 T37426

Product Introduction
Bioactivity


英文名: FIIN-1

描述: FIIN-1 (FGFR irreversible inhibitor-1) 是一种不可逆具有选择性的 FGFR 抑制剂，对 FGFR1、FGFR2、FGFR3、FGFR4、 Flt1、Flt14 的 Kd 分别为 2.8、6.9、5.4、120 ，32和120 nM。FIIN-1 对FGFR1、FGFR2、FGFR3和FGFR4 具有抑制作用， IC50 分别是 9.2，6.2，11.9 和 189 nM。

体外活性: FIIN-1 (14 nM-46 μM; 72 h; ) inhibits the proliferation of FGF signaling-sensitive cancer cell lines. The EC50s of 70 nM, 230 nM, 2.3 μM, for Bladder RT4, Pancreas A2.1, Bone RD-ES cells. EC50s of 0.22 and 4.6 μM for Ovary A2780 and PA-1 cells, respectively. EC50s of 0.08 and 4.5 μM for Lung SBC-3 and H520 cells, respectively. EC50s of 0.14 and 1.65 μM for Kidney G-401 and G-402 cells, respectively. EC50s of 0.014, 0.03, and 0.65 μM for Stomach KATO III, SNU-16, and FU97 cells, respectively.[1]FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely.[1]FIIN-1 binds to BLK, ERK5, KIT, MET, PDGFRB, and VEGFR2 with Kds of 65 nM, 160, 420, 1000, 480, and 210 nM, respectively. The IC50s for Blk and Flt1 are 381 nM and 661 nM respectively.[1]

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

溶解度: DMSO : 45 mg/mL (68.53 mM)


关键字: FIIN 1 | FIIN-1 | FIIN1

相关产品: FGFR4-IN-14 | CP-547632 hydrochloride | Orantinib | FGFR1 inhibitor-9 | PP58 | Dovitinib lactate | S6K2-IN-1 | FGFR4-IN-8 | PD-089828 | KHS101 hydrochloride

相关库: Membrane Protein-targeted Compound Library | Anti-Lung Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Covalent Inhibitor Library | Bioactive Compound 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