Fisogatinib
作者：齊岳
發布時間：2023-08-29
13:38:18
點擊數：
產品名稱：Fisogatinib
產品描述：
| 產品描述 | BLU-554 is a potent inhibitor of fibroblast growth factor receptor 4 (FGFR4). |
| 靶點活性 | FGFR4:5 nM |
| 體外活性 | BLU-554 exploits a unique interaction with FGFR4 to confer potency and selectivity |
| 體內活性 | BLU-554 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models[1]. |
| 激酶實驗 | The Ki value and mode of inhibition of LY2801653 for the MET kinase activity are determined using a radiometric filter-binding assay. Reactions are carried out in 96-well plates in Enzyme dilution buffer (EDB) compose of 50 mM Tris HCl pH 7.5, 2 mM DTT, 0.005% Triton X-100, 10 mM MgCl2, and 250 ?M EDTA. Serially diluted LY2801653 (final concentration 250 to 0 nM) are followed by the addition of a series of 8 concentrations of 33P-γ-ATP (final concentration 400 to 10 μM ATP), and 5 nM enzyme (final concentration). After a 2-hour incubation, PolyGluTyr synthetic protein substrate (final 150 μg/mL) is added to initiate the 30-minute kinase reaction. Reactions are quenched with 10% H3PO4, transfer to a pre-wetted Multiscreen anionic phosphocellulose 96-well filter plate, and washed; radioactivity is measured with a scintillation counter. The experimental data are fit to a global mix model inhibition equation using GraphPad Prism softwar to generate an alpha value to determine the modality of inhibition and to calculate the Ki value for LY2801653[1]. |
| 別名 | BLU554, BLU 554, BLU-554 |
| 分子量 | 503.38 |
| 分子式 | C24H24Cl2N4O4 |
| CAS No. | 1707289-21-1 |
存儲
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 2 mg/mL (3.97 mM)
DMSO: 93 mg/mL (184.8 mM)
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介紹：
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。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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