Lometrexol

Name: Lometrexol
Brand: TargetMol
SKU: T15826
Price: -2 USD
Availability: InStock
Rating: 4.5 (1 reviews)

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.

Catalog No. T15826Cas No. 106400-81-1

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Purity:99.35%

ee:100%

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COA CSFC HNMR HPLC LCMS

Lometrexol

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

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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].
Alias	LY 264618, DDATHF

Chemical Properties

Molecular Weight	443.45
Formula	C₂₁H₂₅N₅O₆
Cas No.	106400-81-1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

5% DMSO+40% PEG300+5% Tween 80+50% Saline: 5 mg/mL, Sonication is recommended. Working solution is recommended to be prepared and used immediately.

DMSO: 100 mg/ml (225.50 mM), Sonication is recommended.

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 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% 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 μLddH2O 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