| Identification | Back Directory | [Name]
FIIN-2 | [CAS]
1633044-56-0 | [Synonyms]
FIN-2
FIIN-2
CS-1618
FIIN2;FIIN-2;FIIN 2
inhibit,FGFR,FIIN2,FIIN 2,Fibroblast growth factor receptor,Inhibitor,FIIN-2
N-[4-[[3-(3,5-Dimethoxyphenyl)-3,4-dihydro-7-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-2-oxopyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl]phenyl]-2-propenamide
2-Propenamide, N-[4-[[3-(3,5-dimethoxyphenyl)-3,4-dihydro-7-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-2-oxopyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl]phenyl]- | [Molecular Formula]
C35H38N8O4 | [MDL Number]
MFCD28386553 | [MOL File]
1633044-56-0.mol | [Molecular Weight]
634.73 |
| Chemical Properties | Back Directory | [density ]
1.306±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥31.75 mg/mL in DMSO; insoluble in H2O; ≥3.39 mg/mL in EtOH with gentle warming | [form ]
solid | [pka]
13.51±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
FIIN-2 is an irreversible FGFR inhibitor with IC50 values of 3.09, 4.3, 27, and 45.3 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. It has been shown to inhibit cell proliferation of transformed Ba/F3 cell lines and demonstrates antiproliferative activity in cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2. By inhibiting FGFR in a zebrafish developmental model, FIIN-2 caused mild to severe alterations in tail morphogenesis similar to the phenotypes reported following genetic knockdown of FGFR. | [Uses]
FIIN 2 is FGFR inhibitor. It can be used in biological study of DFG-out mode of inhibition by an irreversible Type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors | [in vivo]
Treatment of fish in the embryonic state with either FIIN-2 causes defects to the posterior mesoderm similar to the phenotypes reported following genetic knockdown of FGFR or treatment with other reported FGFR inhibitors. FIIN-2 causes mild or severe phenotypes to the tail morphogenesis in all treated embryonic zebrafish[1]. | [IC 50]
FGFR1: 3.1 nM (IC50); FGFR2: 4.3 nM (IC50); FGFR3: 27 nM (IC50); FGFR4: 45 nM (IC50) | [storage]
Store at -20°C | [References]
[1] LI TAN. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2014, 111 45: E4869-77. DOI: 10.1073/pnas.1403438111 |
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| Company Name: |
Twochem Co.Ltd.
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| Telephone: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
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