| Bioactivity | Lometrexol (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. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor[1][2][3]. |
| Invitro | Lometrexol (DDATHF) hydrate binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides[3]. Lometrexol (1-30 μM; 2-10 hours) hydrate induces rapid and complete growth inhibition in L1210 cells[3].Lometrexol (1 μM; 2-24 hours) hydrate induces cell cycle arrest in murine leukemia L1210 cells[3]. Cell Viability Assay[3] Cell Line: |
| Name | Lometrexol hydrate |
| CAS | 1435784-14-7 |
| Formula | C21H27N5O7 |
| Molar Mass | 461.47 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Lometrexol hydrate
CAS: 1435784-14-7 F: C21H27N5O7 W: 461.47
Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltran
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