Powder: -20°C for 3 years | In solvent: -80°C for 1 year
hVEGF-IN-1 是一种喹唑啉衍生物,可以特异性结合内部核糖体进入位点 A 中富含 G 的序列,并会使 G-四链体结构不稳定。在 SPR 实验中,它与 IRES-A (WT) 结合的Kd 值为 0.928 μM。它能够抑制VEGF-A 蛋白表达,阻止肿瘤细胞迁移,抑制肿瘤生长。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 937 | 现货 | ||
5 mg | ¥ 2,230 | 现货 | ||
10 mg | ¥ 3,160 | 现货 | ||
25 mg | ¥ 5,220 | 现货 | ||
50 mg | ¥ 7,380 | 现货 | ||
100 mg | ¥ 9,930 | 现货 | ||
500 mg | ¥ 19,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,330 | 现货 |
产品描述 | hVEGF-IN-1 inhibits human VEGF-A translation and has antitumor activity. |
体外活性 | hVEGF-IN-1 has a markedly selective interaction with the G-rich region within the 5′-UTR of hVEGF-A mRNA and destabilizes the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) (Kd: 0.928 μM) and binds to the hairpin DNA (Kd: 21.2 μM). The G-rich sequence G774-G790 within the IRES-A of hVEGF-A's 5′-UTR is critical for the translation initiation activity of IRES-A. hVEGF-IN-1 hinders BG4 from binding to the IRES-A RNA G-quadruplex in cells. hVEGF-IN-1 down-regulates the translation of hVEGF-A via the G-quadruplex within IRES-A mRNA. hVEGF-IN-1 reduces MDA-MB- 231 cell migration to about 25%. |
体内活性 | In tumor-bearing mice, hVEGF-IN-1 causes an average tumor volume of fewer than 300 mm3. In the presence of hVEGF-IN-1, the tumor weight reduces around 60.1% to a final weight of 0.18 g and no obvious change in body weight. |
细胞实验 | MDA-MB-231 cells are plated in the top chambers of 0.8 μm pore trans-wells in Opti-MEM reduced serum medium in the presence or absence of hVEGF-IN-1. Meanwhile, 600 μL of DMEM containing 10% fetal bovine serum (FBS) and 100 μM CoCl2 are added to the lower chambers. The cells are allowed to migrate for 24 h. At the end of the assay, the cells in the top chamber are removed, and the cells at the bottom of the filter are treated by adding 500 μL of DMEM containing 2.5 mg/mL MTT to each well. After incubating at 37 °C with 5% CO2 for 4 h, 500 μL of DMSO is added to each well and the plate is gently rotated for 10 min. Absorbance (570 nm) is measured using a microplate reader. |
动物实验 | Mice are separated into three groups: negative control, compound 1-treated, and positive control (doxorubicin-treated). hVEGF-IN-1, doxorubicin, and saline are administered by intraperitoneal injection to athymic nude mice with human tumor xenografts established using MCF-7 breast cancer cells. Mice are injected intraperitoneal once a day for 20 days. Negative controls are injected with 150 μL of saline. The positive control group received doxorubicin by intraperitoneal injection at a dose of 1 mg/kg. hVEGF-IN-1 is similarly administered to mice at a dose of 7.5 mg/kg. After treating the animals for 20 days, the tumor tissues are collected and IHC assays are conducted using an anti-VEGF-A antibody[1]. |
分子量 | 581.75 |
分子式 | C34H43N7O2 |
CAS No. | 1637443-98-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.82 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.719 mL | 8.5948 mL | 17.1895 mL | 42.9738 mL |
5 mM | 0.3438 mL | 1.719 mL | 3.4379 mL | 8.5948 mL | |
10 mM | 0.1719 mL | 0.8595 mL | 1.719 mL | 4.2974 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。
hVEGF-IN-1 1637443-98-1 Angiogenesis Tyrosine Kinase/Adaptors VEGFR Inhibitor quinazoline IRES-A migration hVEGF IN 1 hVEGFIN1 tumor G-rich inhibit Vascular endothelial growth factor receptor VEGF-A inhibitor