Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SU 5402 是多靶点受体酪氨酸激酶抑制剂,能够抑制VEGFR2 (IC50:20 nM),FGFR1 (IC50:30 nM),PDGFRβ (IC50:510 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 221 | 现货 | ||
5 mg | ¥ 493 | 现货 | ||
10 mg | ¥ 663 | 现货 | ||
25 mg | ¥ 1,330 | 现货 | ||
50 mg | ¥ 2,560 | 现货 | ||
100 mg | ¥ 3,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 543 | 现货 |
产品描述 | SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively. |
靶点活性 | PDGFRβ:510 nM, FGFR1:30 nM, VEGFR2:20 nM |
体外活性 | SU5402 inhibits VEGF-, FGF-, PDGF- dependent cell proliferation with IC50 of 0.05 μM, 2.80 μM, 28.4 μM, respectively. [1] In HUVECs, SU5416 selectively inhibits VEGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 μM. [2] In nasopharyngeal epithelial cells, SU5402 attenuates LMP1-mediated aerobic glycolysis, cellular transformation, cell migration, and invasion. [3] In mouse C3H10T1/2 cells, SU 5402 diminishes the effect of FGF23 on cell differentiation. [4] |
体内活性 | In mice, SU5416 (25 mg/kg, i.p.) inhibits subcutaneous growth of a panel of tumor cell lines by inhibiting the angiogenic process associated with tumor growth. [2] |
激酶实验 | FGF-R1 and Flk-1/KDR kinase assays.: The catalytic portion of FGF-R1 and Flk-1/KDR are expressed as GST fusion proteins following infection of Spodoptera frugiperda (sf9) cells with engineered baculoviruses. GST-FGFR1 and GST-Flk1 are purified to homogeneity from infected sf9 cell lysates by glutathione sepharose chromatography. The assays are performed in 96-well microtiter plates that had been coated overnight with 2.0 μg of a polyGlu-Tyr peptide (4:1) in 0.1 mL of PBS per well. The purified kinases are diluted in kinase assay buffer (100 mM Hepes pH 7.5, 100 mM NaCl, and 0.1 mM sodium orthovanadate) and added to all test wells at 5 ng of GST fusion protein per 0.05 mL volume buffer. Test compounds are diluted in 4% DMSO and added to test wells (0.025 mL/well). The kinase reaction is initiated by the addition of 0.025 mL of 40 μM ATP/40 mM MnCl2, and plates are shaken for 10 min before stopping the reactions with the addition of 0.025 mL of 0.5 M EDTA. The final ATP concentration was 10 μM, which is twice the experimentally determined Km value for ATP. Negative control wells receive MnCl2 alone without ATP. The plates are washed three times with 10 mM Tris pH 7.4, 150 mM NaCl, and 0.05% Tween-20 (TBST). Rabbit polyclonal anti-phosphotyrosine antiserum is added to the wells at a 1:10000 dilution in TBST for 1 h. The plates are then washed three times with TBST. Goat anti-rabbit antiserum conjugated with horseradish peroxidase was then added to all wells for 1 h. The plates are washed three times with TBST, and the peroxidase reaction is detected with the addition of 2,2‘-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS). The color readout of the assay is allowed to develop for 20?30 min and read on a Dynatech MR5000 ELISA plate reader using a 410 nM test filter. |
细胞实验 | Tumor cell lines used in the in vitro growth are cultured in media at 37°C in 5–10% CO2. SU5416 is serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture. Cell growth is measured after 96 h using the sulforhodamine B method. IC50s are calculated by curve fitting using four-parameter analysis.(Only for Reference) |
别名 | SU5402 |
分子量 | 296.32 |
分子式 | C17H16N2O3 |
CAS No. | 215543-92-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 29.6 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.3747 mL | 16.8737 mL | 33.7473 mL | 84.3683 mL |
5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL | 16.8737 mL | |
10 mM | 0.3375 mL | 1.6874 mL | 3.3747 mL | 8.4368 mL | |
20 mM | 0.1687 mL | 0.8437 mL | 1.6874 mL | 4.2184 mL | |
50 mM | 0.0675 mL | 0.3375 mL | 0.6749 mL | 1.6874 mL | |
100 mM | 0.0337 mL | 0.1687 mL | 0.3375 mL | 0.8437 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。
SU 5402 215543-92-3 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR PDGFR inhibit Inhibitor Fibroblast growth factor receptor SU5402 Platelet-derived growth factor receptor SU-5402 Vascular endothelial growth factor receptor inhibitor