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KI8751

KI8751

产品编号 T2446   CAS 228559-41-9

Ki8751 是一种有效的 VEGFR2 抑制剂,其 IC50=0.9 nM。

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KI8751 Chemical Structure
KI8751, CAS 228559-41-9
规格 价格/CNY 货期 数量
2 mg ¥ 237 现货
5 mg ¥ 418 现货
10 mg ¥ 733 现货
25 mg ¥ 1,330 现货
50 mg ¥ 2,260 现货
100 mg ¥ 3,780 现货
200 mg ¥ 5,430 现货
500 mg ¥ 8,380 现货
1 mL * 10 mM (in DMSO) ¥ 432 现货
产品目录号及名称: KI8751 (T2446)
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纯度: 99.9%
纯度: 99.73%
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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 KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
靶点活性 VEGFR2:0.9 nM
体外活性 在LC-6细胞的裸鼠异种移植模型中,Ki8751(5 mg/kg)在不影响体重的情况下完全抑制肿瘤生长.在携带人类肿瘤异种移植物GL07,St-4,LC6,DLD-1和A375细胞的裸鼠中,Ki8751(20 mg/kg)抑制肿瘤生长.
体内活性 在人脐静脉内皮细胞(HUVECs)中,Ki8751(1 nM-100 nM)有效降低VEGF刺激的细胞增殖和血管通透性。在转移性结直肠癌(CRC)细胞MIP,RKO,SW620和SW480中,Ki8751(10 nM)增加细胞衰老,但在HCT116中无此效果。Ki8751有效且选择性抑制VEGFR-2,IC50为0.9 nM。Ki8751也抑制PDGFRα,c-Kit和 FGFR-2,具有更高的IC50值为40 nM–170 nM。
激酶实验 Cellular Kinase Assays: NIH3T3 cells prepared by transfection of human KDR. The cells are cultured in a collagen type I coated 96-well plate in an amount of 1.5 × 104 per well. The medium is then replaced by a DMEM medium containing 0.1% FCS. Ki8751 diluted in DMSO is added to each well and cultured. rhVEGF is added to a final concentration of 100 ng/mL, and the stimulation of cells is carried out at 37 °C. The cells are washed with PBS (pH 7.4), 50 μL of a solubilization buffer (20 mM HEPES (pH 7.4), 150 mM NaCl, 0.2% Triton X-100, 10% glycerol, 5 mM Na3VO4, 5 mM disodium ethylenediamine tetraacetate, and 2 mM Na4P2O7) is then added and a cell extract is prepared. Separately, PBS (50 μL, pH 7.4) containing 5 μg/mL of antiphosphotyrosine antibody (PY20) is added to a microplate for ELISA. After washing of the plate, 300 μL of a blocking solution is added. The cell extract is transferred to the plate. An anti-VEGFR2 antibody and a peroxidase-labeled anti-rabbit Ig antibody are added. Next, a chromophoric substrate for peroxidase is added, and the absorbance at 450 nm is measured with microplate reader. The VEGFR2 phosphorylation activity for each well is determined by presuming the absorbance with the addition of VEGF and without the addition of the test sample to be 100% VEGFR2 phosphorylation activity and VEGF to be 0% VEGFR2 phosphorylation activity. The concentration of the inhibition (%) of VEGFR2 Phosphorylation is determined for each case, and IC50 value is calculated.
细胞实验 To evaluate the inhibition of VEGF-Stimulated HUVEC proliferation by Ki8751, HUVECs are plated at a density of 4000 cells/200 μL/well in a type I collagen pre-coated 96-well plates. After 24 hours, the cells are incubated for 1 hour with Ki8751 and then stimulated with 20 ng/mL rhVEGF. The cultures are incubated at 37 °C for 72 hours, then pulsed with 1 μCi/well [3H]thymidine and re-incubated for 14 hours. Cells are assayed for the incorporation of tritium using a beta counter. (Only for Reference)
分子量 469.41
分子式 C24H18F3N3O4
CAS No. 228559-41-9

存储

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

溶解度

DMSO: 46.9 mg/mL (100 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 2.1303 mL 10.6517 mL 21.3033 mL 53.2583 mL
5 mM 0.4261 mL 2.1303 mL 4.2607 mL 10.6517 mL
10 mM 0.213 mL 1.0652 mL 2.1303 mL 5.3258 mL
20 mM 0.1065 mL 0.5326 mL 1.0652 mL 2.6629 mL
50 mM 0.0426 mL 0.213 mL 0.4261 mL 1.0652 mL
100 mM 0.0213 mL 0.1065 mL 0.213 mL 0.5326 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Kubo K, et al. J Med Chem, 2005, 48(5), 1359-1366. 2. Tamura D, et al. Cancer Sci, 2010, 101(6), 1403-1408. 3. Hasan MR, et al. Int J Cancer, 2011, 129(9), 2115–2123.
Imatinib Sorafenib tosylate AXL-IN-13 Nintedanib esylate KG5 Axitinib Sunitinib-d10 Multi-kinase inhibitor 1

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 细胞重编程化合物库 抑制剂库 血管生成库 抗结直肠癌化合物库 激酶抑制剂库 成骨分子库 抗卵巢癌化合物库 JAK-STAT 化合物库 抗肺癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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计算 重置

技术支持

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。

Keywords

KI8751 228559-41-9 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR VEGFR FGFR PDGFR c-Kit inhibit KI-8751 KI 8751 Ki 8751 Inhibitor Vascular endothelial growth factor receptor inhibitor

 

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