Antifolate

Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells.

Pemetrexed is a novel antifolate with multiple targets

Nolatrexed Dihydrochloride is an antifolate thymidylate synthase inhibitor.

Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.

Pelitrexol is a GARFT inhibitor, and is also a water soluble antifolate with anti-proliferative activity.

LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.

LY 222306 is a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor with a Ki of 0.77 nM.

LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.