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

Lometrexol (Synonyms: DDATHF)

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

Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) by tightly binding with it. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity.

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 Get quote
1 mg USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 830 Get quote
10 mg USD 1395 Get quote
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Based on 1 publication(s) in Google Scholar

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Description

Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) by tightly binding with it. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity[1].

IC50 & Target

Antifolate and GARFT[1]

In Vitro

Lometrexol (DDATHF) induces abnormal proliferation and apoptosis exist in neural tube defects (NTDs)[1].
Lometrexol significantly reduces the expression of PH3[1].

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].

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

Purity: 99.20%

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Keywords:

LometrexolDDATHFAntifolateApoptosisantipurineantifolateGARFTnovopurinesynthesiscellproliferationapoptosiscyclearrestanticancerInhibitorinhibitorinhibit

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Lometrexol
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