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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
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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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $521 | In Stock | |
| 25 mg | $1,530 | 8-10 weeks | |
| 50 mg | $1,990 | 8-10 weeks | |
| 100 mg | $3,310 | 8-10 weeks | |
| 1 mL x 10 mM (in DMSO) | $631 | 8-10 weeks |
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Purity:98.03%
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Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| Alias | 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 & Solubility Information
| 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. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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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 . A total of 10 animals were administered, and the formula you used is 5% 
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 (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.
(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 main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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