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FIIN-2

Catalog No. T6836   CAS 1633044-56-0

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.

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FIIN-2 Chemical Structure
FIIN-2, CAS 1633044-56-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 35.00
2 mg In stock $ 48.00
5 mg In stock $ 88.00
10 mg In stock $ 157.00
25 mg In stock $ 305.00
50 mg In stock $ 547.00
100 mg In stock $ 779.00
1 mL * 10 mM (in DMSO) In stock $ 139.00
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Purity: 99.65%
Purity: 99.34%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
Targets&IC50 FGFR4:45.3 nM, FGFR3:27 nM, FGFR1:3.09 nM, FGFR2:4.3 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]
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

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)

TargetMolReferences and Literature

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

TargetMolCitations

1. Yang Y L, Cao L B, He W R, et al. Endocytosis triggers V-ATPase-SYK–mediated priming of cGAS activation and innate immune response. Proceedings of the National Academy of Sciences. 2022, 119(43): e2207280119.

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library Inhibitor Library Highly Selective Inhibitor Library Tyrosine Kinase Inhibitor Library Covalent Inhibitor Library Cytokine Inhibitor Library Angiogenesis related Compound Library Anti-Cancer Compound Library Anti-Breast Cancer Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

FIIN-2 1633044-56-0 Angiogenesis Tyrosine Kinase/Adaptors FGFR inhibit FIIN 2 Fibroblast growth factor receptor Inhibitor FIIN2 inhibitor

 

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