ZM323881
(Synonyms: ZM 323881;ZM-323881) 目录号 : GC12656
A potent and selective VEGFR2 inhibitor
Cas No.:193001-14-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
ZM323881 inhibits VEGF-A-induced endothelial cell proliferation (IC50 = 8 nM) and VEGF-R2 tyrosine phosphorylation (IC50 < 2 nM).
Vascular endothelial growth factor (VEGF) increases vascular permeability and angiogenesis in many pathological conditions, such as cancer, arthritis, and diabetes. VEGF activates VEGF-Receptor 1 (VEGF-R1) and VEGF-Receptor 2 (VEGF-R2) that autophosphorylate to initiate a signaling cascade resulting in angiogenesis and increased microvascular permeability. ZM323881 is a potent and selective inhibitor of VEGF-R2 tyrosine kinase.
In vitro: ZM323881 was found to inhibit VEGF-A-induced endothelial cell proliferation (IC50 = 8 nM) and VEGF-R2 tyrosine phosphorylation in vitro (IC50 < 2 nM) [1].
In vivo: VEGF-Amediated increases in vascular permeability in perfused mesenteric microvessels in vivo were reversibly abolished by both ZM323881 and the class III receptor tyrosine kinase inhibitor PTK787/ZK222584, suggesting that VEGF-R2 phosphorylation is necessary for VEGF-A-mediated increases in microvascular permeability in vivo [1].
Clinical trials: There is no clinical data are available currenlty.
Reference:
[1] Whittles CE, Pocock TM, Wedge SR, Kendrew J, Hennequin LF, Harper SJ, Bates DO. ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity. Microcirculation. 2002;9(6):513-22.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6638 mL | 13.3191 mL | 26.6383 mL |
| 5 mM | 0.5328 mL | 2.6638 mL | 5.3277 mL |
| 10 mM | 0.2664 mL | 1.3319 mL | 2.6638 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。