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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.
| Molecular Weight | 443.45 |
| Formula | C21H25N5O6 |
| CAS Number | 106400-81-1 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Antifolate Products |
|---|
| Pemetrexed disodium
Pemetrexed is a novel antifolic acid antimetabolic compound with K I of 1.3 nM, 7.2 nM, and 65 nM for TS, DHFR, and GARFT, respectively. |
| Methotrexate
Methotrexate (Amethopterin) is an antimetabolite and antifolate agent with antineoplastic and immunosuppressant activities. |
| Folinic acid calcium salt
Folic acid is an adjuvant compound used in cancer chemotherapy. *The compound is unstable in solutions, freshly prepared is recommended |
| Sulfamethazine
Sulfamethazine is a sulfonamide antibacterial. |
| Pyrimethamine
Pyrimethamine is a dihydrofolate reductase(DHFR) inhibitor with an IC50 of 15.4 nM. |
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