FIIN-2
作者：齊岳
發(fā)布時間：2023-08-25
09:06:54
點擊數(shù)：
產(chǎn)品名稱：FIIN-2
產(chǎn)品描述：
| 產(chǎn)品描述 | 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. |
| 靶點活性 | FGFR4:45.3 nM, FGFR3:27 nM, FGFR1:3.09 nM, FGFR2:4.3 nM |
| 體外活性 | 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] |
| 體內(nèi)活性 | In a zebrafish developmental model, FIIN-2 causes mild or severe phenotypes to the tail morphogenesis by inhibiting FGFR. [1] |
| 激酶實驗 | Biochemical assays: Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform. |
| 細胞實驗 | 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) |
| 分子量 | 634.741 |
| 分子式 | C35H38N8O4 |
| CAS No. | 1633044-56-0 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
Ethanol: <1 mg/mL
DMSO: 64 mg/mL (100.8 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業(yè)務范圍包括化學試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學品、中間體和化工材料等領域。
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