ZD-4190

Modify Date: 2024-01-09 13:22:24

ZD-4190 Structure
ZD-4190 structure
Common Name ZD-4190
CAS Number 413599-62-9 Molecular Weight 459.272
Density 1.6±0.1 g/cm3 Boiling Point 583.2±60.0 °C at 760 mmHg
Molecular Formula C19H16BrFN6O2 Melting Point N/A
MSDS N/A Flash Point 306.5±32.9 °C

 Use of ZD-4190


ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.

 Names

Name N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-[2-(1H-1,2,3-triazol-1-yl)ethoxy]-4-quinazolinamine
Synonym More Synonyms

 ZD-4190 Biological Activity

Description ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
Related Catalog
Target

EGFR

VEGFR2

In Vitro ZD4190 exhibits cytotoxic activity against the tumor cells[2].
In Vivo ZD4190 (100 mg/kg, p.o.) effectively delays MDA-MB-435 tumor growth in mice. In ZD4190-treated tumors, 18F-FPPRGD2 uptake has decreased significantly relative to baseline by 26.74±8.12% (p<0.05) on day 1 and by 41.19±6.63% (p<0.01) on day 3, then has returned to baseline on day 7. Tumor uptake of 18F-FLT has also decreased on both day 1 and day 3 after initiation of ZD4190 treatment. However, ZD4190 does not significantly change 18F-FDG uptake in tumors, compared with the control group[1]. ZD4190 (50 mg/kg, p.o.) prevents outgrowth of residual tumour in a muscle model of minimal residual carcinoma[2]. ZD4190 (12.5-100 mg/kg, p.o.) produces a dose-dependent reduction in K(trans) in PC-3 prostate tumors. At 100 mg/kg, ZD4190 reduces K(trans) in PC-3 tumors by 31% following 2 doses and by 53% following 8 doses[3].
Cell Assay The cytotoxicity of ZD4190 for PDVC57B cells is established when 104 cells are exposed to 1-10 μM ZD4190 for 96 h before MTS solution is added and the optical density measured at 490 nm. Cells are also grown to 40% confluence and treated with 1-100 μM ZD4190 for 7 days and the cytopathic effect examined by staining with crystal violet.
Animal Admin ZD4190 is suspended in a 1% (v/v) solution of polyoxyethylene sorbitan mono-oleate in deionized water and administered by oral gavage (0.1 mL/10 g body weight). In each experiment, mice are randomized to receive either vehicle or ZD4190, administered once daily using a 1 day (at 0 and 22 h) or 7 day (at 0, 24, 48, 72, 96, 120, 144, and 166 h) treatment regimen (i.e., daily administration of compound for 1 or 7 days with an additional dose given 2 h prior to the end of the treatment period) followed by DCEMRI under terminal anesthesia.
References

[1]. Yang M, et al. PET imaging of early response to the tyrosine kinase inhibitor ZD4190. Eur J Nucl Med Mol Imaging. 2011 Jul;38(7):1237-47. doi: 10.1007/s00259-011-1742-z. Epub 2011 Mar 1.

[2]. Gaballah K, et al. The antiangiogenic agent ZD4190 prevents tumour outgrowth in a model of minimal residual carcinoma in deep tissues. Br J Cancer. 2009 Aug 4;101(3):418-23. doi: 10.1038/sj.bjc.6605092. Epub 2009 Jul 21.

[3]. Checkley D, et al. Dynamic contrast-enhanced MRI of vascular changes induced by the VEGF-signalling inhibitor ZD4190 in human tumour xenografts. Magn Reson Imaging. 2003 Jun;21(5):475-82.

 Chemical & Physical Properties

Density 1.6±0.1 g/cm3
Boiling Point 583.2±60.0 °C at 760 mmHg
Molecular Formula C19H16BrFN6O2
Molecular Weight 459.272
Flash Point 306.5±32.9 °C
Exact Mass 458.050201
LogP 4.16
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.688
Storage condition 2-8℃

 Synonyms

N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[2-(1H-1,2,3-triazol-1-yl)ethoxy]quinazolin-4-amine
N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-[2-(1H-1,2,3-triazol-1-yl)ethoxy]-4-quinazolinamine
4-Quinazolinamine, N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[2-(1H-1,2,3-triazol-1-yl)ethoxy]-
ZD-4190
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