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hVEGF-IN-1

hVEGF-IN-1

产品编号 T4288   CAS 1637443-98-1

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。

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hVEGF-IN-1 Chemical Structure
hVEGF-IN-1, CAS 1637443-98-1
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: hVEGF-IN-1 (T4288)
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 5.82 mg/mL (10 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Discovery of Small Molecules for Repressing Cap-Independent Translation of Human VascularEndothelial Growth Factor (hVEGF) as Novel Antitumor Agents. J Med Chem. 2017 Jul 13;60(13):5306-5319.
ENMD-2076 VEGFR2-IN-1 Vorolanib ZM323881 hydrochloride R1530 Telatinib TG 100572 BMS-2

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 抑制剂库 激酶抑制剂库 NO PAINS 化合物库 细胞因子抑制剂库 抗前列腺癌化合物库 抗纤维化化合物库 抗胰腺癌化合物库 抗癌化合物库 经典已知活性库

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Keywords

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

 

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