3-[5-[2-[(2-Methoxyethyl)methylamino]ethoxy]-1H-indol-2-yl]-2(1H)-quinolinone
- Product Name
- 3-[5-[2-[(2-Methoxyethyl)methylamino]ethoxy]-1H-indol-2-yl]-2(1H)-quinolinone
- CAS No.
- 408502-06-7
- Chemical Name
- 3-[5-[2-[(2-Methoxyethyl)methylamino]ethoxy]-1H-indol-2-yl]-2(1H)-quinolinone
- Synonyms
- KDR-in-4;VEGFR-2-IN-9;VEGFR 2 IN 9,VEGFR2IN9;3-[5-[2-[(2-Methoxyethyl)methylamino]ethoxy]-1H-indol-2-yl]-2(1H)-quinolinone;2(1H)-Quinolinone, 3-[5-[2-[(2-methoxyethyl)methylamino]ethoxy]-1H-indol-2-yl]-
- CBNumber
- CB63339581
- Molecular Formula
- C23H25N3O3
- Formula Weight
- 391.4629
- MOL File
- 408502-06-7.mol
3-[5-[2-[(2-Methoxyethyl)methylamino]ethoxy]-1H-indol-2-yl]-2(1H)-quinolinone Property
- Melting point:
- 204-205 °C
- Boiling point:
- 651.5±55.0 °C(Predicted)
- Density
- 1.235±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 11.55±0.70(Predicted)
3-[5-[2-[(2-Methoxyethyl)methylamino]ethoxy]-1H-indol-2-yl]-2(1H)-quinolinone Chemical Properties,Usage,Production
Uses
VEGFR-2-IN-9 (KDR-in-4) is a potent kinase insert domain-containing receptor (KDR/VEGFR2) inhibitor with an IC50 of 7 nM.
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].
IC 50
KDR: 7 nM (IC50)
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. DOI:10.1021/jo062228w
[2] Kinose F, et al. Inhibition of retinal and choroidal neovascularization by a novel KDR kinase inhibitor. Molecular Vision 2005; 11:366-373