ZD-4190

SKU: orb1220938

Description

ZD-4190 is a 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.

Key Properties

• CAS Number: 413599-62-9
• MW: 459.28
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₆BrFN₆O₂
• SMILES: COc1cc2c(Nc3ccc(Br)cc3F)ncnc2cc1OCCn1ccnn1
• Target: EGFR
• Solubility: DMSO:20.83 mg/mL (45.35 mM)

Bioactivity

• 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. ZD4190 (50 mg/kg, p.o.) prevents outgrowth of residual tumour in a muscle model of minimal residual carcinoma. 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.
• In Vitro:
  ZD4190 exhibits cytotoxic activity against the tumor cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

EGFR