1. Cell Cycle/DNA Damage
    Apoptosis
  2. Antifolate
    Apoptosis
  3. Lometrexol

Lometrexol (Synonyms: DDATHF)

Cat. No.: HY-14521
Handling Instructions

Lometrexol (DDATHF), 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.

For research use only. We do not sell to patients.

Lometrexol Chemical Structure

Lometrexol Chemical Structure

CAS No. : 106400-81-1

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10 mM * 1 mL in DMSO USD 810 Ask For Quote & Lead Time
1 mg USD 275 Ask For Quote & Lead Time
5 mg USD 830 Ask For Quote & Lead Time
10 mg USD 1395 Ask For Quote & Lead Time

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Description

Lometrexol (DDATHF), 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[1][2]. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor[3].

IC50 & Target

GARFT[1]

In Vitro

Lometrexol (DDATHF) binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides[2].
Lometrexol (1-30 μM; 2-10 hours) induces rapid and complete growth inhibition in L1210 cells[2].
Lometrexol (1 μM; 2-24 hours) induces cell cycle arrest in murine leukemia L1210 cells[2].
Lometrexol induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Mouse leukemia L1210 cells
Concentration: 1, 30 μM
Incubation Time: 2, 4, 6, 8, 10 hours
Result: Induced rapid and complete growth inhibition.

Cell Cycle Analysis[2]

Cell Line: L1210 cells
Concentration: 1 μM
Incubation Time: 2, 4, 8, 12, 24 hours
Result: Caused a rapid loss of the G2/M phase population of cells and an early S phase accumulation of cells by 8 hours. By 24 h, the S phase population appeared to be slowly shifting to higher DNA content, and hence, from mid-to-late S phase.
In Vivo

Lometrexol (DDATHF; i.p.; 15-60 mg/kg; on gestation day 7.5) increases the rate of embryonic resorption and growth retardation in a dose-dependent manner[1].
Lometrexol (i.p.; 40 mg/kg) maximally inhibits GARFT activity after at 6 hours and thereafter gradually increases with time but remains significantly lower than control even at 96 hours. Levels of ATP, GTP, dATP and dGTP of NTDs embryonic brain tissue decreases significantly at 6 h, and more significantly over time[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (7-8 week, 18-20 g)[1]
Dosage: 15, 30, 35, 40, 45 and 60 mg/kg
Administration: Intraperitoneal injection; on gestation day 7.5
Result: Increased the rate of embryonic resorption and growth retardation in a dose-dependent manner.
Clinical Trial
Molecular Weight

443.45

Formula

C₂₁H₂₅N₅O₆

CAS No.

106400-81-1

SMILES

O=C1C2=C(NC[[email protected]](CCC3=CC=C(C(N[[email protected]@H](CCC(O)=O)C(O)=O)=O)C=C3)C2)N=C(N)N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (90.20 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2550 mL 11.2752 mL 22.5505 mL
5 mM 0.4510 mL 2.2550 mL 4.5101 mL
10 mM 0.2255 mL 1.1275 mL 2.2550 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

LometrexolDDATHFAntifolateApoptosisantipurineantifolateGARFTnovopurinesynthesiscellproliferationapoptosiscyclearrestleukemiaL1210Inhibitorinhibitorinhibit

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Lometrexol
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