Bioactivity | Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor[1][2][3]. | |||||||||
Invitro | Lometrexol (DDATHF) disodium binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides[3]. Lometrexol (1-30 μM; 2-10 hours) disodium induces rapid and complete growth inhibition in L1210 cells[3].Lometrexol (1 μM; 2-24 hours) disodium induces cell cycle arrest in murine leukemia L1210 cells[3]. Cell Viability Assay[3] Cell Line: | |||||||||
Name | Lometrexol disodium | |||||||||
CAS | 120408-07-3 | |||||||||
Formula | C21H23N5Na2O6 | |||||||||
Molar Mass | 487.42 | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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