408502-06-7
408502-06-7 structure
- Name: KDR-in-4
- Chemical Name: KDR-in-4
- CAS Number: 408502-06-7
- Molecular Formula: C23H25N3O3
- Molecular Weight: 391.46
- Catalog: Research Areas Cardiovascular Disease
- Create Date: 2018-05-24 18:15:42
- Modify Date: 2024-01-13 15:43:06
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KDR-in-4 is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC50 of 7 nM.
| Name | KDR-in-4 |
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| Description | KDR-in-4 is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC50 of 7 nM. |
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| Related Catalog | |
| Target |
KDR:7 nM (IC50) |
| In Vitro | 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]. |
| In Vivo | 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]. |
| Animal Admin | 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 |
| Molecular Formula | C23H25N3O3 |
|---|---|
| Molecular Weight | 391.46 |