FIIN-1 是一种有效的，不可逆的选择性FGFR抑制剂。FIIN-1 与FGFR1/2/3/4和Flt1/4结合，Kd分别为 2.8/6.9/5.4/120 nM 和 32/120 nM。FIIN-1 抑制 FGFR1/2/3/4 的IC50分别是 9.2，6.2，11.9 和 189 nM。
| 生物活性 | FIIN-1 is a potent, irreversible, selectiveFGFRinhibitor. FIIN-1 binds toFGFR1/2/3/4andFlt1/4withKds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemicalIC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively[1]. |
| IC50& Target[1] | FGFR1 2.8 nM (Kd) | FGFR2 6.9 nM (Kd) | FGFR3 5.4 nM (Kd) | FGFR4 120 nM (Kd) | FGFR1 9.2 nM (IC50) | FGFR2 6.2 nM (IC50) | FGFR3 11.9 nM (IC50) | FGFR4 189 nM (IC50) |
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体外研究
(In Vitro) | FIIN-1 binds to BLK, ERK5, KIT, MET, PDGFRB and VEGFR2 with Kds of 65 nM, 160, 420, 1000, 480 and 210 nM, respectively. The IC50s for Blk and Flt1 are 381 nM and 661 nM respectively[1].
FIIN-1 (14 nM-46 μM; 72 hours) inhibits proliferation of FGF signaling-sensitive cancer cell lines[1].
FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely.
Cell Proliferation Assay[1] | Cell Line: | Stomach KATO III, SNU-16 and FU97 cells; Bladder RT4 cells; Kidney G-401 and G-402 cells; Lung SBC-3 and H520 cells; Pancreas A2.1 cells; Ovary A2780 and PA-1 cells; Bone RD-ES cells | | Concentration: | | | Incubation Time: | 72 hours | | Result: | The EC50of 70 nM for Bladder RT4 cell.
The EC50of 230 nM for Pancreas A2.1 cell.
The EC50of 2.3 μM for Bone RD-ES cell.
EC50s of 0.22 and 4.6 μM for Ovary A2780 and PA-1 cells, respectively.
EC50s of 0.08 and 4.5 μM for Lung SBC-3 and H520 cells, respectively.
EC50s of 0.14 and 1.65 μM for Kidney G-401 and G-402 cells, respectively.
EC50s of 0.014, 0.03 and 0.65 μM for Stomach KATO III, SNU-16, FU97 cells, respectively. |
Western Blot Analysis[1] | Cell Line: | Serum-starved MCF10A cells that stably express iFGFR1 | | Concentration: | 20 nM | | Incubation Time: | 30 minutes | | Result: | Blocked activation of iFGFR1 and phosphorylation of downstream effectors Erk1/2. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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