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Lometrexol

Name: Lometrexol
Brand: TargetMol
SKU: T15826
Price: 81 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15826Cas No. 106400-81-1

Alias LY 264618, DDATHF

Lometrexol (LY 264618), an antipurine Antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and Apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

Lometrexol

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Purity: 99.56%

Catalog No. T15826Alias LY 264618, DDATHFCas No. 106400-81-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$81	In Stock	In Stock
5 mg	$198	In Stock	In Stock
10 mg	$328	In Stock	In Stock
25 mg	$562	In Stock	In Stock
50 mg	$829	-	In Stock
100 mg	$1,150	-	In Stock
200 mg	$1,530	10-14 weeks	10-14 weeks
1 mL x 10 mM (in DMSO)	$226	In Stock	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. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.56%

ee:100%

Appearance:Solid

Color:White

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COA HNMR CSFC LCMS

Product Introduction

Bioactivity

Description	Lometrexol (LY 264618), an antipurine Antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and Apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
In vitro	Lometrexol binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides. Lometrexol (1-30 μM; 2-10 hours) induces rapid and complete growth inhibition in L1210 cells. Lometrexol (1 μM; 2-24 hours) induces cell cycle arrest in murine leukemia L1210 cells[3].
In vivo	Lometrexol (DDATHF; i.p.; 15-60 mg/kg; on gestation day 7.5) induces neural tube defects (NTDs) by disrupting purine metabolism, increasing embryonic resorption rates, and causing growth retardation in a dose-dependent manner. At 40 mg/kg, it decreases glycinamide ribonucleotide formyl transferase (GARFT) activity and alters ATP, GTP, dATP, and dGTP levels. Additionally, Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) leads to abnormal cell proliferation and apoptosis in NTDs[1].
Synonyms	LY 264618, DDATHF

Chemical Properties

Molecular Weight	443.45
Formula	C₂₁H₂₅N₅O₆
Cas No.	106400-81-1
Smiles	Nc1nc2NC[C@H](CCc3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)Cc2c(=O)[nH]1
Relative Density.	1.56 g/cm3 (Predicted)

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: 100 mg/mL (225.5 mM), Sonication is recommended.

In Vivo Formulation

5% DMSO+40% PEG300+5% Tween 80+50% Saline: 5 mg/mL (11.28 mM), Solution.

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	2.2550 mL	11.2752 mL	22.5505 mL	112.7523 mL
5 mM	0.4510 mL	2.2550 mL	4.5101 mL	22.5505 mL
10 mM	0.2255 mL	1.1275 mL	2.2550 mL	11.2752 mL
20 mM	0.1128 mL	0.5638 mL	1.1275 mL	5.6376 mL
50 mM	0.0451 mL	0.2255 mL	0.4510 mL	2.2550 mL
100 mM	0.0226 mL	0.1128 mL	0.2255 mL	1.1275 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 stock solution preparation method and in vivo formula preparation method:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent 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 TargetMol | 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.

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