ZD-4190

Cat. No.: HY-U00002 Purity: 98.08%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 413599-62-9

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 303	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 303	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 460	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 990	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1400	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

EGFR

VEGFR2

In Vitro

ZD4190 exhibits cytotoxic activity against the tumor cells^[2].

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

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].

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

Molecular Weight

459.27

Formula

C₁₉H₁₆BrFN₆O₂

CAS No.

413599-62-9

Appearance

Solid

Color

White to off-white

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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 20.83 mg/mL (45.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.08%

Select Batch:

Data Sheet (279 KB) SDS (0 KB)

COA (254 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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	[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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1774 mL	10.8868 mL	21.7737 mL	54.4342 mL
	5 mM	0.4355 mL	2.1774 mL	4.3547 mL	10.8868 mL
	10 mM	0.2177 mL	1.0887 mL	2.1774 mL	5.4434 mL
	15 mM	0.1452 mL	0.7258 mL	1.4516 mL	3.6289 mL
	20 mM	0.1089 mL	0.5443 mL	1.0887 mL	2.7217 mL
	25 mM	0.0871 mL	0.4355 mL	0.8709 mL	2.1774 mL
	30 mM	0.0726 mL	0.3629 mL	0.7258 mL	1.8145 mL
	40 mM	0.0544 mL	0.2722 mL	0.5443 mL	1.3609 mL

ZD-4190 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZD-4190413599-62-9ZD4190ZD 4190VEGFREGFRVascular endothelial growth factor receptorEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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