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

LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM for human GARFT and also has high affinity at human folate receptor (FR)α and FRβ (Ki, 1.78 nM and 18.2 nM, respectively). LY309887 is signigicantly cytotoxic against the human leukemia cell line CCRF-CEM with IC50 of 9.9 nM[1].

LY309887 (3 mg/kg-100 mg/kg, i.p.) shows complete inhibition on the tumor growth in mice bearing C3H mammary cancer cells[1].

[1]. Mendelsohn LG, et al. Biochemistry and pharmacology of glycinamide ribonucleotide formyltransferase inhibitors: LY309887 and lometrexol. Invest New Drugs. 1996;14(3):287-94.

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