product name FIIN-2
Description: FIIN-2 is a potent, selective, irreversible pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively. FIIN-2 is the first class of inhibitors that can potently inhibit the proliferation of cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2. Compared with FIIN-1, FIIN-2 displayed strong binding to FGFRs and exhibited good overall kinase selectivity.
References: Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-77.
634.73
Formula
C35H38N8O4
CAS No.
1633044-56-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 69 mg/mL (108.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19420363
| In Vitro |
In vitro activity: 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. Kinase Assay: Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform. Cell Assay: 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. |
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| In Vivo | In a zebrafish developmental model, FIIN-2 causes mild or severe phenotypes to the tail morphogenesis by inhibiting FGFR. |
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| Formulation & Dosage | |
| References | Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-77. |
