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Gartisertib

Name: Gartisertib
Brand: TargetMol
SKU: T10407
Price: 129 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

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

🥰Excellent

Purity: 99.52%

Catalog No. T10407Alias VX-803, VX 03, VRT1228692, M4344, M 4344, ATR inhibitor 2Cas No. 1613191-99-3

Pack Size	Price	USA Warehouse	Global Warehouse
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. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.52%

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COA HPLC HNMR FNMR

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]
Synonyms	VX-803, VX 03, VRT1228692, M4344, M 4344, ATR inhibitor 2

Chemical Properties

Molecular Weight	541.55
Formula	C₂₅H₂₉F₂N₉O₃
Cas No.	1613191-99-3
Smiles	O=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

Storage

Powder: -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 recommeded.

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

	1mg	5mg	10mg	50mg
1 mM	1.8466 mL	9.2328 mL	18.4655 mL	92.3276 mL
5 mM	0.3693 mL	1.8466 mL	3.6931 mL	18.4655 mL
10 mM	0.1847 mL	0.9233 mL	1.8466 mL	9.2328 mL
20 mM	0.0923 mL	0.4616 mL	0.9233 mL	4.6164 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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