LY 254155 ?binds to membrane folate-binding protein (mFBP) [1] and inhibits recombinant human monofunctional glycinamide ribonucleotide formyltransferase (hGARFT).

LY 254155 (5, 10, 20, and 40 mg/kg) inhibits murine C3H carcinoma growth in C3H mice, with % inhibition of tumor growth is 49%, 71%, 90%, and 94%, respectively[1].LY 254155 is active against a broad panel of murine and human xenograft solid tumors.