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Gartisertib

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Catalog No. T10407Cas No. 1613191-99-3
Alias VX-803, VX 03, VRT1228692, M4344, M 4344, ATR inhibitor 2

Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.

Gartisertib

Gartisertib

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Purity: 99.52%
Catalog No. T10407Alias VX-803, VX 03, VRT1228692, M4344, M 4344, ATR inhibitor 2Cas No. 1613191-99-3
Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$129-In Stock
5 mg$322-In Stock
10 mg$538-In Stock
25 mg$1,070-In Stock
50 mg$1,570-In Stock
100 mg$2,360-In Stock
1 mL x 10 mM (in DMSO)$383-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.52%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.
Targets&IC50
ATR:8 nM
In vitro
Gartisertib was four times more potent in all glioblastoma cell lines than the widely used ATR inhibitor berzosertib (Gartisertib median IC50 = 0.56 μM, berzosertib median IC50 = 2.21 μM). In addition, Gartisertib observed a higher IC50 (7.22 μM) in human astrocytes, indicating a lower potential toxicity of Gartisertib to normal brain cells.
The combination of Gartisertib (1 μM) with TMZ+RT significantly increased apoptosis and cell death in patient-derived glioblastoma cell lines. [1]
In vivo
Gartisertib (10 mg/kg or 20 mg/kg) plus cisplatin inhibited tumor growth in metastatic clear cell renal cell carcinoma (ccRCC) xenografts, demonstrating therapeutic synergies. [2]
SynonymsVX-803, VX 03, VRT1228692, M4344, M 4344, ATR inhibitor 2
Chemical Properties
Molecular Weight541.55
FormulaC25H29F2N9O3
Cas No.1613191-99-3
SmilesO=C(NC=1C=NC=C(F)C1N2CCC(C(=O)N3CCN(CC3)C4COC4)CC2)C=5C(=NN6C=C(F)C=NC56)N
Relative Density.1.31g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 16 mg/mL (29.54 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Saline: 1.5 mg/mL (2.77 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8466 mL9.2328 mL18.4655 mL92.3276 mL
5 mM0.3693 mL1.8466 mL3.6931 mL18.4655 mL
10 mM0.1847 mL0.9233 mL1.8466 mL9.2328 mL
20 mM0.0923 mL0.4616 mL0.9233 mL4.6164 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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