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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $35 | In Stock | |
2 mg | $48 | In Stock | |
5 mg | $64 | In Stock | |
10 mg | $98 | In Stock | |
25 mg | $208 | In Stock | |
50 mg | $317 | In Stock | |
1 mL x 10 mM (in DMSO) | $91 | In Stock |
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. |
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] |
Kinase Assay | Biochemical assays: Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform. |
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) |
Molecular Weight | 634.73 |
Formula | C35H38N8O4 |
Cas No. | 1633044-56-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 64 mg/mL (100.8 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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