Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PD173074 是一种 FGFR1抑制剂,IC50为 25 nM。它也可抑制 VEGFR2活性,IC50值为 100-200 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 196 | 现货 | ||
5 mg | ¥ 438 | 现货 | ||
10 mg | ¥ 653 | 现货 | ||
25 mg | ¥ 1,280 | 现货 | ||
50 mg | ¥ 2,390 | 现货 | ||
100 mg | ¥ 3,630 | 现货 | ||
200 mg | ¥ 5,260 | 现货 | ||
500 mg | ¥ 8,170 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 525 | 现货 |
产品描述 | 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. |
靶点活性 | FGFR1:25 nM, VEGFR2:100 nM-200 nM |
体外活性 | 在KMS11异种移植瘤模型中,PD173074抑制FGFR3造成的肿瘤生长延缓,提高小鼠存活率. 在H-510异种移植体中,PD173074与顺铂阻断肿瘤生长的作用相似,与对照组相比中位生存期增加.在H-69异种移植体中,PD173074对50%小鼠的诱导作用大于6个月.PD173074(1/2 mg/kg/day)剂量依赖性地有效阻止由成纤维生长因子或血管内皮生长因子诱导的小鼠血管生成,且无明显毒性.在裸鼠体内,PD173074对NIH 3T3细胞(成纤维细胞生长因子受体3突变体转染)生长有抑制作用. |
体内活性 | PD173074剂量依赖性地抑制VEGFR2(IC50:100-200 nM)和FGFR1(IC50:1-5 nM)的自身磷酸化。 PD173074剂量依赖性抑制FGF-2促进的颗粒神经元存活(IC50:12 nM),比SU 5402活性高1,000倍以上。 PD173074对FGF-2-介导的少突胶质细胞谱系细胞的细胞增殖、分化及MAPK激活具有特异性的抑制作用。PD173074是ATP竞争性的FGFR1抑制剂(Ki:40 nM)。PD173074还剂量依赖性地有效抑制FGFR3的自磷酸化(IC50:5 nM)。在多发性骨髓瘤细胞系中,PD173074对野生型及FGFR3突变型有活性。PD173074使表达FGFR3的KMS11细胞和KMS18细胞的活力显著下降(IC50<20 nM)。 |
激酶实验 | 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. |
细胞实验 | 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 | 523.67 |
分子式 | C28H41N7O3 |
CAS No. | 219580-11-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 52.4 mg/mL (100 mM)
DMSO: 52.4 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 1.9096 mL | 9.548 mL | 19.096 mL | 47.74 mL |
5 mM | 0.3819 mL | 1.9096 mL | 3.8192 mL | 9.548 mL | |
10 mM | 0.191 mL | 0.9548 mL | 1.9096 mL | 4.774 mL | |
20 mM | 0.0955 mL | 0.4774 mL | 0.9548 mL | 2.387 mL | |
50 mM | 0.0382 mL | 0.191 mL | 0.3819 mL | 0.9548 mL | |
100 mM | 0.0191 mL | 0.0955 mL | 0.191 mL | 0.4774 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PD173074 219580-11-7 Angiogenesis Apoptosis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR VEGFR FGFR IGF-1R Src Inhibitor Fibroblast growth factor receptor PD 173074 Vascular endothelial growth factor receptor inhibit PD-173074 inhibitor