| Bioactivity | Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor[1][2][3]. | ||||||||||||
| Invitro | Lometrexol (DDATHF) binds tightly to GART, resulting in a rapid and prolonged depletion of intracellular purine ribonucleotides[3]. Lometrexol (1-30 μM; 2-10 hours) induces rapid and complete growth inhibition in L1210 cells[3].Lometrexol (1 μM; 2-24 hours) induces cell cycle arrest in murine leukemia L1210 cells[3]. Cell Viability Assay[3] Cell Line: | ||||||||||||
| Name | Lometrexol | ||||||||||||
| CAS | 106400-81-1 | ||||||||||||
| Formula | C21H25N5O6 | ||||||||||||
| Molar Mass | 443.45 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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Lometrexol
CAS: 106400-81-1 F: C21H25N5O6 W: 443.45
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase
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