Chemical Property of FIIN-3
Chemical Property:
- Boiling Point:909.4±65.0 °C(Predicted)
- PKA:10.78±0.70(Predicted)
- PSA:124.19000
- Density:1.379±0.06 g/cm3(Predicted)
- LogP:6.88110
- Purity/Quality:
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99%, *data from raw suppliers
FIIN-?3 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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Useful:
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Description
FIIN-3 is an inhibitor of FGF receptors (FGFRs; IC50s = 13, 21, 31, and 35 nM for recombinant FGFR1-4, respectively). It is selective for FGFRs over a panel of 456 kinases at a concentration of 1 μM, however, it does inhibit EGFR (IC50 = 204 nM). FIIN-3 inhibits growth of Ba/F3 cells that are dependent on the kinase activity of wild-type FGFR1-4 as well as gatekeeper mutant FGFR2 and FGFR3 (EC50s = <1-69 nM) and inhibits FGFR-dependent signaling in a concentration-dependent manner in FGFR2TEL/V564M-dependent Ba/F3 cells. FIIN-3 also inhibits growth in a panel of cancer cell lines (EC50s = 1.4-499 nM).
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Uses
FIIN-?3 is FGFR inhibitor. It can be used in synthetic preparation and complex with EGFR kinase of crystal structure; development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.