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Lometrexol

Catalog No. T15826 CAS 106400-81-1

Synonyms: DDATHF, LY 264618

Lometrexol, an antipurine <a href="/target/Antifolate" style="display: inline; color: #c13a36">Antifolate</a>, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of <a href="/target/DNA" style="display: inline; color: #c13a36">DNA</a> strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and <a href="/pathway/Apoptosis" style="display: inline; color: #c13a36">Apoptosis</a>, even <a href="/target/cell_cycle_arrest" style="display: inline; color: #c13a36">cell cycle arrest</a>. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

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Lometrexol, CAS 106400-81-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 253.00
5 mg	In stock	$ 752.00
10 mg	In stock	$ 1,261.00
25 mg	In stock	$ 1,861.00
50 mg	In stock	$ 2,788.00
100 mg	In stock	$ 4,183.00
1 mL * 10 mM (in DMSO)	In stock	$ 827.00

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Purity: 98.57%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Lometrexol, 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 disturbing purine metabolism and increases the rate of embryonic resorption and growth retardation in a dose-dependent manner. Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) decreases glycinamide ribonucleotide formyl transferase (GARFT) activity and Changes of ATP, GTP, dATP and dGTP levels[1]. Lometrexol (i.p.; 40 mg/kg; on gestation day 7.5) induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs)[1].

Synonyms	DDATHF, LY 264618
Molecular Weight	443.45
Formula	C21H25N5O6
CAS No.	106400-81-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 36mg/mL (81.2mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Xu L, et al. The effect of inhibiting glycinamide ribonucleotide formyl transferase on the development of neural tube in mice. Nutr Metab (Lond). 2016 Aug 23;13(1):56. 2. Scaletti E, et, al. Structural basis of inhibition of the human serine hydroxymethyltransferase SHMT2 by antifolate drugs. FEBS Lett. 2019 Jul;593(14):1863-1873. 3. Bronder JL, et, al. Antifolates targeting purine synthesis allow entry of tumor cells into S phase regardless of p53 function. Cancer Res. 2002 Sep 15;62(18):5236-41.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Lung Cancer Compound Library Bioactive Compounds Library Max Anti-Cancer Active Compound Library Bioactive Compound Library

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Pralatrexate Trioxsalen Fanotaprim Brodimoprim WR99210 Managlinat dialanetil Pelitrexol ZD 7155(hydrochloride)

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Keywords

Lometrexol 106400-81-1 Cell Cycle/Checkpoint DNA Damage/DNA Repair Metabolism DHFR DDATHF LY 264618 Inhibitor inhibitor inhibit

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