PD173074
作者：齊岳
發布時間：2023-08-25
09:00:18
點擊數：
產品名稱：PD173074
產品描述：
| 產品描述 | PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src. |
| 靶點活性 | FGFR1:25 nM, VEGFR2:100 nM-200 nM |
| 體外活性 | 在KMS11異種移植瘤模型中,PD173074抑制FGFR3造成的生長延緩,提高小鼠存活率. 在H-510異種移植體中,PD173074與順鉑阻斷生長的作用相似,與對照組相比中位生存期增加.在H-69異種移植體中,PD173074對50％小鼠的誘導作用大于6個月.PD173074（1/2 mg/kg/day）劑量依賴性地有效阻止由成纖維生長因子或血管內皮生長因子誘導的小鼠血管生成,且無明顯毒性.在裸鼠體內,PD173074對NIH 3T3細胞（成纖維細胞生長因子受體3突變體轉染）生長有抑制作用. |
| 體內活性 | PD173074劑量依賴性地抑制VEGFR2（IC50：100-200 nM）和FGFR1（IC50：1-5 nM）的自身磷酸化。 PD173074劑量依賴性抑制FGF-2促進的顆粒神經元存活（IC50：12 nM）,比SU 5402活性高1,000倍以上。 PD173074對FGF-2-介導的少突膠質細胞譜系細胞的細胞增殖、分化及MAPK激活具有特異性的抑制作用。PD173074是ATP競爭性的FGFR1抑制劑（Ki：40 nM）。PD173074還劑量依賴性地有效抑制FGFR3的自磷酸化（IC50：5 nM）。在多發性骨髓瘤細胞系中,PD173074對野生型及FGFR3突變型有活性。PD173074使表達FGFR3的KMS11細胞和KMS18細胞的活力顯著下降（IC50<20 nM）。 |
| 激酶實驗 | In vitro kinase inhibition assays: Assays using the full-length FGFR-1 kinase are performed in a total volume of 100 μL containing 25 mM HEPES buffer (pH 7.4), 150 mM NaCl, 10 mM MnCl2, 0.2 mM sodium orthovanadate, 750 μg/mL concentration of a random copolymer of glutamic acid and tyrosine (4:1), various concentrations of PD173074 and 60 to 75 ng of enzyme. The reaction is initiated by the addition of [γ-32P]ATP (5 μM ATP containing 0.4 μCi of [γ-32P]ATP per incubation), and samples are incubated at 25°C for 10 minutes. The reaction is terminated by the addition of 30% trichloroacetic acid and the precipitation of material onto glass-fiber filter mats. Filters are washed three times with 15% trichloroacetic acid, and the incorporation of [32P] into the glutamate tyrosine polymer substrate is determined by counting the radioactivity retained on the filters in a Wallac 1250 betaplate reader. Nonspecific activity is defined as radioactivity retained on the filters following incubation of samples without enzyme. Specific activity is determined as total activity (enzyme plus buffer) minus nonspecific activity. The concentration of PD173074 that inhibits FGFR-1 enzymatic activity by 50% (IC50) is determined graphically. |
| 細胞實驗 | Cells are incubated with increasing concentrations of PD173074 in the presence of aFGF/heparin for 48 hours. The percentage of viable cells is determined by MTT.(Only for Reference) |
| 分子量 | 523.682 |
| 分子式 | C28H41N7O3 |
| CAS No. | 219580-11-7 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 52.4 mg/mL (100 mM)
DMSO: 52.4 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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