Fisogatinib
作者：齐岳
发布时间：2023-08-29
13:38:18
点击数：
产品名称：Fisogatinib
产品描述：
| 产品描述 | BLU-554 is a potent inhibitor of fibroblast growth factor receptor 4 (FGFR4). |
| 靶点活性 | FGFR4:5 nM |
| 体外活性 | BLU-554 exploits a unique interaction with FGFR4 to confer potency and selectivity |
| 体内活性 | BLU-554 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models[1]. |
| 激酶实验 | 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]. |
| 别名 | BLU554, BLU 554, BLU-554 |
| 分子量 | 503.38 |
| 分子式 | C24H24Cl2N4O4 |
| CAS No. | 1707289-21-1 |
存储
| 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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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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