1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. KDR-in-4

KDR-in-4 

Cat. No.: HY-101628
Handling Instructions

KDR-in-4 is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC50 of 7 nM.

For research use only. We do not sell to patients.

KDR-in-4 Chemical Structure

KDR-in-4 Chemical Structure

CAS No. : 408502-06-7

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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.

IC50 & Target[1]

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].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

391.46

Formula

C₂₃H₂₅N₃O₃

CAS No.

408502-06-7

SMILES

O=C1NC2=C(C=CC=C2)C=C1C(N3)=CC4=C3C=CC(OCCN(CCOC)C)=C4

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
KDR-in-4
Cat. No.:
HY-101628
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KDR-in-4

Cat. No.: HY-101628