FIIN-2

SKU: orb1300421

Description

FIIN-2 is an irreversible pan-FGFR inhibitor exhibiting potent activity against FGFR1-4 with IC50 values of 3.09, 4.3, 27, and 45.3 nM, respectively. It is a valuable chemical probe for studying FGFR-driven pathologies in both cellular assays and preclinical cancer models.

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1633044-56-0
MW	634.73
Purity	99.34%
Formula	C₃₅H₃₈N₈O₄
SMILES	COc1cc(OC)cc(c1)N1Cc2cnc(Nc3ccc(cc3)N3CCN(C)CC3)nc2N(Cc2ccc(NC(=O)C=C)cc2)C1=O
Target	FGFR
Solubility	H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:64 mg/mL (100.83 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.15 mM)

Bioactivity

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Target IC50	FGFR2:4.3 nM\|FGFR4:45.3 nM\|FGFR3:27 nM\|FGFR1:3.09 nM
In Vivo	In a zebrafish developmental model, FIIN-2 causes mild or severe phenotypes to the tail morphogenesis by inhibiting FGFR.
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. Read more...
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) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Inhibitor, Fibroblast growth factor receptor, FGFR2, FGFR, FGFR1, FGFR4, FGFR3, FIIN 2, FIIN2, FIIN-2, inhibit

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Compound Identifiers

PubChem CID

91825767 ↗

Key Properties

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No computed properties available.

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FIIN-2 (orb1300421)

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Purity:	>98% (HPLC)
CAS Number:	1633044-56-0
MW:	634.73
Formula:	C₃₅H₃₈N₈O₄

FIIN-2

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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