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Pelitrexol

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Catalog No. T14147Cas No. 446022-33-9
Alias AG2037, AG 2037

Pelitrexol (AG2037) is a GARFT inhibitor, which can inhibit the activity of mTORC1, reduce intracellular guanine nucleotides and block the cell cycle in the s-phase, with antiproliferative activity, and can be used in non-small cell lung cancer.

Pelitrexol

Pelitrexol

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Purity: 98.03%
Catalog No. T14147Alias AG2037, AG 2037Cas No. 446022-33-9
Pelitrexol (AG2037) is a GARFT inhibitor, which can inhibit the activity of mTORC1, reduce intracellular guanine nucleotides and block the cell cycle in the s-phase, with antiproliferative activity, and can be used in non-small cell lung cancer.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$5218-10 weeks8-10 weeks
25 mg$1,5308-10 weeks8-10 weeks
50 mg$1,9908-10 weeks8-10 weeks
100 mg$3,3108-10 weeks8-10 weeks
1 mL x 10 mM (in DMSO)$6318-10 weeks8-10 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.03%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Pelitrexol (AG2037) is a GARFT inhibitor, which can inhibit the activity of mTORC1, reduce intracellular guanine nucleotides and block the cell cycle in the s-phase, with antiproliferative activity, and can be used in non-small cell lung cancer.
Targets&IC50
mTORC1:27-40 nM
In vitro
Pelitrexol potently inhibits mTORC1 signaling (IC₅₀ ≈ 27-40 nM) in NSCLC cells, causes G1 arrest, and acts via GARFT inhibition. The effects of Pelitrexol are reversed by hypoxanthine, confirming target specificity[1].
In vivo
In a mouse xenograft model of non-small-cell lung cancer (NSCLC), intraperitoneal administration of Pelitrexol at 10 mg/kg or 20 mg/kg every 4 days for 3 weeks reduced tumor growth by 64% and 69%, respectively. At 20 mg/kg, it also suppressed mTORC1-dependent phosphorylation of S6K1, S6RP, and CAD, confirming disruption of purine biosynthesis via GARFT inhibition[1].
SynonymsAG2037, AG 2037
Chemical Properties
Molecular Weight463.51
FormulaC20H25N5O6S
Cas No.446022-33-9
SmilesO=C1C2=C(NC[C@@H](CCC=3SC(C(N[C@@H](CCC(O)=O)C(O)=O)=O)=CC3C)C2)NC(N)=N1
Relative Density.1.64g/cm3
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 20 mg/mL (43.15 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (4.31 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 mM2.1575 mL10.7873 mL21.5745 mL107.8725 mL
5 mM0.4315 mL2.1575 mL4.3149 mL21.5745 mL
10 mM0.2157 mL1.0787 mL2.1575 mL10.7873 mL
20 mM0.1079 mL0.5394 mL1.0787 mL5.3936 mL

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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:
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