FIIN-2

Catalog No.S7714 Batch:S771401

Technical Data

Formula	C₃₅H₃₈N₈O₄
Molecular Weight	634.73	CAS No.	1633044-56-0
Solubility (25°C)*	In vitro	DMSO	69 mg/mL (108.7 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

FIIN-2 is an 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.

Targets

FGFR1 ^[1] (Cell-free assay)	FGFR2 ^[1] (Cell-free assay)	FGFR3 ^[1] (Cell-free assay)	FGFR4 ^[1] (Cell-free assay)
3.09 nM	4.3 nM	27 nM	45.3 nM

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]

Protocol (from reference)

Kinase Assay:^{^[1]}	Biochemical assays Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform.
Cell Assay:^{^[1]}	Cell lines NCI-H2077, NCI-H1581, H520, Kato III, AN3CA, RT112, A2780, 4T1, and SKOV-3 cells Concentrations 1.0 μM Incubation Time 96 h Method 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.

Kinase Assay:^{^[1]}

Biochemical assays
Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform.

Cell Assay:^{^[1]}

Cell lines
NCI-H2077, NCI-H1581, H520, Kato III, AN3CA, RT112, A2780, 4T1, and SKOV-3 cells
Concentrations
1.0 μM
Incubation Time
96 h
Method
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.

References

[1] Tan L, et al. Proc Natl Acad Sci U S A. 2014, 111(45), E4869-4877.

Selleck's FIIN-2 has been cited by 5 publications

Pregranulosa cell-derived FGF23 protects oocytes from premature apoptosis during primordial follicle formation by inhibiting p38 MAPK in mice [ J Biol Chem, 2023, 299(6):104776]	PubMed: 37142227
Inhibition of autophagy potentiates the cytotoxicity of the irreversible FGFR1-4 inhibitor FIIN-2 on lung adenocarcinoma [ Cell Death Dis, 2022, 13(8):750]	PubMed: 36042213
Cisplatin Resistance in Osteosarcoma: In vitro Validation of Candidate DNA Repair-Related Therapeutic Targets and Drugs for Tailored Treatments. [ Front Oncol, 2020, 10;10:331]	PubMed: 32211337
Expanding the Arsenal of FGFR Inhibitors: A Novel Chloroacetamide Derivative as a New Irreversible Agent With Anti-proliferative Activity Against FGFR1-Amplified Lung Cancer Cell Lines. [ Front Oncol, 2019, 9:179]	PubMed: 30972293
Expanding the Arsenal of FGFR Inhibitors: A Novel Chloroacetamide Derivative as a New Irreversible Agent With Anti-proliferative Activity Against FGFR1-Amplified Lung Cancer Cell Lines [ Front Oncol, 2019, 9:179]	PubMed: 30972293

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SHIPPING AND STORAGE
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