Description | LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (Ki: 6.5 nM). It also has antitumor activity. |
In vitro | LY309887 is significantly cytotoxic against the human leukemia cell line CCRF-CEM (IC50: 9.9 nM). LY309887 also has high affinity at human folate receptor (FR)α and FRβ (Ki, 1.78 nM, and 18.2 nM, respectively) . |
In vivo | In mice bearing C3H mammary cancer cells, LY309887 (3 mg/kg-100 mg/kg, i.p.) displays complete inhibition on the tumor growth. |
Target activity | GARFT:(ki)6.5 nM, FRβ:18.2 nM(ki), FRα:1.78 nM(ki) |
molecular weight | 449.48 |
Molecular formula | C19H23N5O6S |
CAS | 127228-54-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
References | 1. Mendelsohn LG, et al. Biochemistry and pharmacology of glycinamide ribonucleotide formyltransferase inhibitors: LY309887 and lometrexol. Invest New Drugs. 1996;14(3):287-94. |