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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $521 | 8-10 weeks | 8-10 weeks | |
| 25 mg | $1,530 | 8-10 weeks | 8-10 weeks | |
| 50 mg | $1,990 | 8-10 weeks | 8-10 weeks | |
| 100 mg | $3,310 | 8-10 weeks | 8-10 weeks | |
| 1 mL x 10 mM (in DMSO) | $631 | 8-10 weeks | 8-10 weeks |
| 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]. |
| Synonyms | AG2037, AG 2037 |
| Molecular Weight | 463.51 |
| Formula | C20H25N5O6S |
| Cas No. | 446022-33-9 |
| Smiles | O=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 | store 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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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