Lometrexol

SKU: orb1707028

Description

Lometrexol (LY 264618) is an antipurine antifolate that potently inhibits glycinamide ribonucleotide formyltransferase (GARFT) and human serine hydroxymethyltransferase (hSHMT1/2), disrupting de novo purine synthesis. This activity leads to suppressed cell proliferation, cell cycle arrest, and apoptosis, underpinning its research use as an anticancer agent in both in vitro and in vivo studies.

Research Area

Cell Biology, Metabolism Research, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 106400-81-1
• MW: 443.45
• Purity: 99.56% (May vary between batches)
• Formula: C₂₁H₂₅N₅O₆
• SMILES: Nc1nc2NC[C@H](CCc3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)Cc2c(=O)[nH]1
• Target: Antifolate,Bcl-2 Family,DHFR,Apoptosis,Caspase
• Solubility: 5% DMSO+40% PEG300+5% Tween 80+50% Saline:5 mg/mL (11.28 mM);DMSO:100 mg/mL (225.5 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LY264618, LY-264618, LY 264618, Lometrexol, GARFT, DDATHF, Antifolate

Compound Identifiers

PubChem CID

135413518