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

Lometrexol hydrate (Synonyms: DDATHF hydrate)

Cat. No.: HY-14521B Purity: 99.20%
Handling Instructions

Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity.

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Lometrexol hydrate Chemical Structure

Lometrexol hydrate Chemical Structure

CAS No. : 1435784-14-7

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Based on 1 publication(s) in Google Scholar

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Description

Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity[1][2].

IC50 & Target

GARFT[1]

In Vitro

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

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 hydrate (DDATHF hydrate; 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 hydrate (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].

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.
Molecular Weight

461.47

Formula

C₂₁H₂₇N₅O₇

CAS No.

1435784-14-7

SMILES

O=C(O)CC[[email protected]@H](C(O)=O)NC(C1=CC=C(CC[[email protected]@H](CN2)CC3=C2N=C(N)NC3=O)C=C1)=O.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: 99.20%

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Keywords:

LometrexolDDATHFAntifolateApoptosisantipurineantifolateGARFTnovopurinesynthesiscellproliferationapoptosiscyclearrestleukemiaL1210Inhibitorinhibitorinhibit

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Lometrexol hydrate
Cat. No.:
HY-14521B
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