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Pelitrexol

Name: Pelitrexol
Brand: TargetMol
SKU: T14147
Rating: 4.5 (1 reviews)

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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

Pack Size	Price	Availability
5 mg	$521	8-10 weeks
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

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

Chemical Properties

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

	1mg	5mg	10mg	50mg
1 mM	2.1575 mL	10.7873 mL	21.5745 mL	107.8725 mL
5 mM	0.4315 mL	2.1575 mL	4.3149 mL	21.5745 mL
10 mM	0.2157 mL	1.0787 mL	2.1575 mL	10.7873 mL
20 mM	0.1079 mL	0.5394 mL	1.0787 mL	5.3936 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.

Dose Conversion

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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