| Name | FIIN-2 |
| Description | 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. |
| Cell Research | 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) |
| Kinase Assay | Biochemical assays: Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform. |
| In vitro | 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] |
| In vivo | In a zebrafish developmental model, FIIN-2 causes mild or severe phenotypes to the tail morphogenesis by inhibiting FGFR. [1] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.15 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 64 mg/mL (100.83 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | FIIN-2 | FIIN2 | FIIN 2 | Fibroblast growth factor receptor | FGFR4 | FGFR3 | FGFR2 | FGFR1 | FGFR |
| Inhibitors Related | Amlexanox | Regorafenib monohydrate | Nintedanib | Ferulic Acid | Nintedanib esylate | Regorafenib | Pemigatinib | Formononetin | Lenvatinib mesylate | Erdafitinib | Lenvatinib | Pazopanib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Osteogenesis Compound Library | Reprogramming Compound Library | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Liver Cancer Compound Library |
United States
