| Identification | Back Directory | [Name]
3-[5-[2-[(2-Methoxyethyl)methylamino]ethoxy]-1H-indol-2-yl]-2(1H)-quinolinone | [CAS]
408502-06-7 | [Synonyms]
KDR-in-4
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]- | [Molecular Formula]
C23H25N3O3 | [MDL Number]
MFCD30747898 | [MOL File]
408502-06-7.mol | [Molecular Weight]
391.463 |
| Chemical Properties | Back Directory | [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) |
| Hazard Information | Back Directory | [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 |
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