KDR-in-4
(Synonyms: KDR-in-4) 目录号 : GC32625
KDR-in-4 (KDR-in-4) 是一种有效的激酶插入结构域受体 (KDR/VEGFR2) 抑制剂，IC50 为 7 nM。
Cas No.:408502-06-7
Sample solution is provided at 25 µL, 10mM.
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KDR-in-4 is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC50 of 7 nM.
KDR (kinase insert domain-containing receptor) is one of the human tyrosine kinases that has a high affinity for vascular endothelial growth factor (VEGF) and is believed to be a primary mediator of tumor-induced angiogenesis[1].
KDR-in-4 may prove to be useful for the treatment of a variety of ocular neovascular diseases using a convenient oral dosing regimen. At doses of 100 mg/kg, KDR-in-4 results in a 98% reduction in lesion size in the rat choroidal neovascularization (CNV) model. 30 mg/kg doses of KDR-in-4 shows a 70% and 80% reduction in lesion size in the laser CNV and rat oxygen induced retinopathy (OIR) models, respectively[2].
[1]. Fang YQ, et al. Efficient syntheses of KDR kinase inhibitors using a Pd-catalyzed tandem C-N/Suzuki coupling as the key step. J Org Chem. 2007 Feb 16;72(4):1341-6. [2]. Kinose F, et al. Inhibition of retinal and choroidal neovascularization by a novel KDR kinase inhibitor. Molecular Vision 2005; 11:366-373
Animal experiment: | Rats: KDR-in-4 is dosed by oral gavage for 12 days at 0, 10, 30, or 100 mg/kg in an adult male Brown Norway rat laser induced choroidal neovascularization (CNV) model. The areas of CNV lesions are quantitated by fluorescence image analysis of FITC-dextran perfused animals. KDR-in-4 is also assessed in a rat oxygen induced retinopathy (OIR) model in which neonatal rats are placed in an oxygen chamber that delivered alternating 24 h cycles of 50% and 10% oxygen for 14 days. After 14 days of oxygen treatment, the animals are returned to room air and dosed orally for 7 days with 0, 10, or 30 mg/kg kinase inhibitor. The extent of retinal neovascularization is assessed by counting pre-retinal neovascular nuclei on histological sections[2]. |
References: [1]. Fang YQ, et al. Efficient syntheses of KDR kinase inhibitors using a Pd-catalyzed tandem C-N/Suzuki coupling as the key step. J Org Chem. 2007 Feb 16;72(4):1341-6. | |
| Cas No. | 408502-06-7 | SDF | |
| 别名 | KDR-in-4 | ||
| Canonical SMILES | O=C1NC2=C(C=CC=C2)C=C1C(N3)=CC4=C3C=CC(OCCN(CCOC)C)=C4 | ||
| 分子式 | C23H25N3O3 | 分子量 | 391.46 |
| 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 | 2.5545 mL | 12.7727 mL | 25.5454 mL |
| 5 mM | 0.5109 mL | 2.5545 mL | 5.1091 mL |
| 10 mM | 0.2555 mL | 1.2773 mL | 2.5545 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet