ZK-261991
目录号 : GC31816
ZK-261991是一种可口服的VEGFR酪氨酸酶抑制剂，抑制VEGFR-2活性的IC50值为5nM。
Cas No.:886563-25-3
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
Cell experiment: | HLMVECs are cultured in EGM 2-MV medium. For the cytotoxicity assay, cells are seeded in 96-well plates in EGM 2-MV medium at a density of 5×103 cells/well. Medium is changed every second day, and cells are cultured until reaching confluence. Then the medium is replaced with serum-free medium containing a tyrosine kinase inhibitor (PTK/ZK or ZK991; concentration 20 nM) and left overnight. Control cells receive the substance vehicle. The next day, cytotoxicity assay (WST-1 based) is performed according to the manufacturer's instructions. Colorimetric analysis is performed with an ELISA reader. Subsequent statistical analysis is performed, and graphs are drawn. The number of wells per group is as follows: PTK/ZK control group, n = 30; PTK/ZK 20 nM, n = 30; ZK991 control group, n = 30; ZK991 20 nM, n = 30. |
Animal experiment: | Before corneal neovascularization, each animal is deeply anesthetized. Three 11-0 nylon sutures are placed intrastromally with two stromal incursions extending over 120°C of corneal circumference each. The outer point of suture placement is chosen near the limbus, and the inner suture point is chosen near the corneal center equidistant from the limbus to obtain standardized angiogenic responses. Sutures are left in place for 14 days. The first treatment group receive the tyrosine kinase inhibitor PTK/ZK (75 mg/kg, orally, twice daily), the second treatment group receive the tyrosine kinase inhibitor ZK991 (50 mg/kg, orally, twice daily), and control mice receive equal amounts of the substance vehicle. After 2 weeks, mice are killed and corneas are prepared. The corneal neovascularization assay includes 22 mice in the control group, 11 mice in the PTK/ZK treatment group, and 11 mice in the ZK991 treatment group. |
References: [1]. Deniz Hos, et al. Inflammatory Corneal (Lymph)angiogenesis Is Blocked by VEGFR-Tyrosine Kinase Inhibitor ZK 261991, Resulting in Improved Graft Survival after Corneal Transplantation. Investigative Ophthalmology & Visual Science May 2008, Vol.49, 1836-1842. | |
ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.
ZK-261991 inhibits cellular receptor autophosphorylation in KDR-PAECs with an IC50 of 2 nM. ZK991 inhibits VEGFR-3 autophosphorylation concentration dependently with an IC50 of 20 nM[1].
ZK991 results in a significantly reduced recruitment of CD11b+ and LYVE-1+ cells into the murine cornea. ZK991 significantly improves the graft survival rate after corneal transplantation[1].
[1]. Deniz Hos, et al. Inflammatory Corneal (Lymph)angiogenesis Is Blocked by VEGFR-Tyrosine Kinase Inhibitor ZK 261991, Resulting in Improved Graft Survival after Corneal Transplantation. Investigative Ophthalmology & Visual Science May 2008, Vol.49, 1836-1842.
| Cas No. | 886563-25-3 | SDF | |
| Canonical SMILES | O=C(NC1=CC2=NN(C)C=C2C=C1)C3=CC=CC=C3NCC4=CC(NC(N(C)C)=O)=NC=C4 | ||
| 分子式 | C24H25N7O2 | 分子量 | 443.5 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2548 mL | 11.274 mL | 22.5479 mL |
| 5 mM | 0.451 mL | 2.2548 mL | 4.5096 mL |
| 10 mM | 0.2255 mL | 1.1274 mL | 2.2548 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。