1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. VEGFR
    EGFR
  3. ZD-4190

ZD-4190 

Cat. No.: HY-U00002 Purity: 99.20%
Handling Instructions

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.

For research use only. We do not sell to patients.

ZD-4190 Chemical Structure

ZD-4190 Chemical Structure

CAS No. : 413599-62-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 715 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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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.

IC50 & Target[1]

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].

Molecular Weight

459.27

Formula

C₁₉H₁₆BrFN₆O₂

CAS No.

413599-62-9

SMILES

COC1=CC2=C(NC3=CC=C(Br)C=C3F)N=CN=C2C=C1OCCN4N=NC=C4

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20.83 mg/mL (45.35 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1774 mL 10.8868 mL 21.7737 mL
5 mM 0.4355 mL 2.1774 mL 4.3547 mL
10 mM 0.2177 mL 1.0887 mL 2.1774 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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ZD-4190
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