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  • 化合物 KI8751|T2446|TargetMol

化合物 KI8751|T2446|TargetMol

KI8751
228559-41-9
￥237 2mg 起订
￥418 5mg 起订
￥733 10mg 起订
上海 更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年
联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 KI8751
英文名称：
KI8751
CAS号：
228559-41-9
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.9%
产品类别：
抑制剂
货号：
T2446

Product Introduction

Bioactivity

名称KI8751
描述KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
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)
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.
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。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 14 mg/mL (29.82 mM), Sonication is recommended.
关键字inhibit | KI-8751 | KI 8751 | Ki 8751 | KI8751 | Inhibitor | VEGFR | Vascular endothelial growth factor receptor
相关产品Lapatinib | Neratinib | Gefitinib | Erlotinib | Osimertinib | Amlexanox | Gilteritinib | Formononetin | Ferulic Acid | Regorafenib | Pazopanib | Sorafenib
相关库抑制剂库 | 抗乳腺癌化合物库 | 经典已知活性库 | 抗癌化合物库 | 已知活性化合物库 | 激酶抑制剂库 | 膜蛋白靶向化合物库 | 酪氨酸激酶分子库 | 共价抑制剂库 | 细胞重编程化合物库
KI8751|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

化合物 KI8751相关厂家报价

  • Ki8751
  • Ki8751
  • 南京百鑫德诺生物科技有限公司
  • 2024-09-26
  • 询价
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