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FIIN2 是一种 FGFR 的不可逆抑制剂,能够抑制 FGFR1 (IC50:3.1 nM),FGFR2 (IC50:4.3 nM),FGFR3 (IC50:27 nM) 和 FGFR4 (IC50:45 nM)。
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FIIN2 是一种 FGFR 的不可逆抑制剂,能够抑制 FGFR1 (IC50:3.1 nM),FGFR2 (IC50:4.3 nM),FGFR3 (IC50:27 nM) 和 FGFR4 (IC50:45 nM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 357 | 现货 | |
2 mg | ¥ 483 | 现货 | |
5 mg | ¥ 662 | 现货 | |
10 mg | ¥ 1,060 | 现货 | |
25 mg | ¥ 2,120 | 现货 | |
50 mg | ¥ 3,180 | 现货 | |
100 mg | ¥ 4,560 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 925 | 现货 |
产品描述 | FIIN-2, an irreversible, pan-FGFR inhibitor, inhibits FGFR1/2/3/4 with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM, respectively. |
靶点活性 | FGFR4:45.3 nM, FGFR3:27 nM, FGFR1:3.09 nM, FGFR2:4.3 nM |
体外活性 | 在FGFR1-4 Ba/F3细胞中,FIIN-2通过EC50值位于单到双位纳摩尔范围内,抑制细胞增殖。FIIN-2还在多种背景下显示出优异的抗增殖活性,包括那些在FGFR1具有看门人突变且依赖FGFR4的细胞系。[1] |
体内活性 | 在斑马鱼发育模型中,FIIN-2 通过抑制表皮生长因子受体(FGFR),导致鱼尾形态发生出现或轻或重的表型。[1] |
激酶实验 | Biochemical assays: Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform. |
细胞实验 | NCI-H2077, NCI-H1581, H520, Kato III, AN3CA, RT112, A2780, 4T1, and SKOV-3 cells are treated with inhibitors 1 d after being plated at a density of 1,500 cells per well in 96-well plates. The gatekeeper mutation cell lines are generated by ectopically overexpressing FGFR1 V561M in either NCI-H2077 or NCI-H1581 cells via lentiviral transduction. Cell survival is assessed at 96 h following the addition of inhibitor using the Cell-Titer-Glo reagent according to the manufacturer's instructions. EC50 values are calculated using GraphPad Prism 5. SKOV-3 cells also are treated in the presence of FGF or EGF ligand. Proliferation measurements were made after 96 h using a luminometer. Data are shown as relative values: The luminescence of cells with indicated inhibitor dose is compared with that of untreated cells.(Only for Reference) |
分子量 | 634.73 |
分子式 | C35H38N8O4 |
CAS No. | 1633044-56-0 |
Smiles | COc1cc(OC)cc(c1)N1Cc2cnc(Nc3ccc(cc3)N3CCN(C)CC3)nc2N(Cc2ccc(NC(=O)C=C)cc2)C1=O |
密度 | 1.306 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 64 mg/mL (100.8 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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