ZD-4190
ZD-4190 Basic information
- Product Name:
- ZD-4190
- Synonyms:
-
- ZD-4190
- ZD-4190;ZD 4190;ZD4190
- 4-Quinazolinamine, N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[2-(1H-1,2,3-triazol-1-yl)ethoxy]-
- Inhibitor,inhibit,Vascular endothelial growth factor receptor,VEGFR,Epidermal growth factor receptor,EGFR,ZD 4190,ErbB-1,HER1,ZD-4190,ZD4190
- 7-(2-(1H-1,2,3-Triazol-1-yl)ethoxy)-N-(4-bromo-2-fluorophenyl)-6-methoxyquinazolin-4-amine
- ZD-4190, 10 mM in DMSO
- ZD-4190 ，S6543
- CAS:
- 413599-62-9
- MF:
- C19H16BrFN6O2
- MW:
- 459.27
- Mol File:
- 413599-62-9.mol
ZD-4190 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : 20.83 mg/mL (45.35 mM);Water : < 0.1 mg/mL (insoluble)
- form
- Solid
- color
- White to off-white
ZD-4190 Usage And Synthesis
Uses
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.
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].
IC 50
EGFR; VEGFR2
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. DOI:10.1007/s00259-011-1742-z
[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. DOI:10.1038/sj.bjc.6605092
[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. DOI:10.1016/s0730-725x(02)00644-6
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