lometrexol hydrate

Lometrexol hydrate (DDATHF hydrate) is an antipurine antifolate compound that inhibits glycinamide ribonucleotide formyltransferase (GARFT) activity without inducing detectable DNA strand breaks. It further disrupts de novo purine synthesis, leading to abnormal cell proliferation, apoptosis, and cell cycle arrest, exhibiting anticancer activity [1] [2]. Additionally, it acts as a potent inhibitor of human Serine hydroxymethyltransferase1/2 (h SHMT1/2) [3].

Lometrexol (LY 264618), 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.

Lometrexol (DDATHF) disodium is a potent inhibitor of human serine hydroxymethyltransferase 1/2 (hSHMT1/2) and antifolate, which reduces the activity of glycinamide ribonucleotide formyltransferase (GARFT) without causing detectable levels of DNA strand breaks. Lometrexol disodium exhibits anticancer effects by inhibiting the de novo synthesis of purines, causing abnormal cell proliferation, apoptosis and cell cycle arrest.