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)。
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.
体外活性
In FGFR1-4 Ba/F3 cells, FIIN-2 inhibits cell proliferation with EC50 in the single- to double-digit nanomolar range. FIIN-2 also shows excellent antiproliferative activity in a variety of backgrounds, including cell lines that have gatekeeper mutations in FGFR1 and that are dependent on FGFR4. [1]
体内活性
In a zebrafish developmental model, FIIN-2 causes mild or severe phenotypes to the tail morphogenesis by inhibiting FGFR. [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)
Cas No.
1633044-56-0
分子式
C35H38N8O4
分子量
634.73
储存和溶解度
Ethanol:<1 mgml
DMSO:64 mg/mL (100.8 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years