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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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

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].

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
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

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Product Name:
ZD-4190
Cat. No.:
HY-U00002
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ZD-4190

Cat. No.: HY-U00002