FIIN-2 structure
|
Common Name | FIIN-2 | ||
|---|---|---|---|---|
| CAS Number | 1633044-56-0 | Molecular Weight | 634.727 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C35H38N8O4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of FIIN-2FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. |
| Name | fiin-2 |
|---|---|
| Synonym | More Synonyms |
| Description | FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. |
|---|---|
| Related Catalog | |
| Target |
FGFR1:3.1 nM (IC50) FGFR2:4.3 nM (IC50) FGFR3:27 nM (IC50) FGFR4:45 nM (IC50) |
| In Vitro | FIIN-2 potently inhibits WT FGFRs (EC50s in the 1- to 93-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 58 nM). FIIN-2 also moderately inhibits EGFR, with an IC50 of 204 nM. FIIN-2 inhibits proliferation of FGFR1-4 Ba/F3 cells with EC50s in the single- to double-digit nanomolar range and are especially potent against FGFR2, with EC50s in the 1-nM range. FIIN-2 shows good potency against gatekeeper mutant V564F[1]. |
| 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]. |
| Cell Assay | TEL-FGFR2–transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentration of the compounds. After 72 h the cells are assessed by MTS tetrazolium assay[1]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C35H38N8O4 |
| Molecular Weight | 634.727 |
| Exact Mass | 634.301575 |
| PSA | 115.40000 |
| LogP | 1.82 |
| Index of Refraction | 1.666 |
| Storage condition | -20℃ |
| N-(4-((3-(3,5-dimethoxyphenyl)-7-((4-(4-methylpiperazin-1-yl)phenyl)amino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)methyl)phenyl)acrylamide |
| FIIN2 |
| 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]- |
| N-(4-{[3-(3,5-Dimethoxyphenyl)-7-{[4-(4-methyl-1-piperazinyl)phenyl]amino}-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl}phenyl)acrylamide |