KDR-in-4 (Synonyms: KDR-in-4) |
| カタログ番号GC32625 |
KDR-in-4 (KDR-in-4) は、7 nM の IC50 を持つ強力なキナーゼ挿入ドメイン含有受容体 (KDR/VEGFR2) 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| 同義語 | KDR-in-4 | ||
| Canonical SMILES | O=C1NC2=C(C=CC=C2)C=C1C(N3)=CC4=C3C=CC(OCCN(CCOC)C)=C4 | ||
| Formula | C23H25N3O3 | M.Wt | 391.46 |
| 溶解度 | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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