LY254155是一种抗叶酸剂。LY254155抑制hGARFT及与mFBP结合，Kis分别为2.1±0.2和1.7±0.1nM。
LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
LY 254155 inhibits recombinant human monofunctional glycinamide ribonucleotide formyltransferase (hGARFT) and binds to membrane folate-binding protein (mFBP) [1].
LY 254155 is active against a broad panel of murine and human xenograft solid tumors. 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].
[1]. Habeck LL, et al. A novel class of monoglutamated antifolates exhibits tight-binding inhibition of humanglycinamide ribonucleotide formyltransferase and potent activity against solid tumors. Cancer Res. 1994 Feb 15;54(4):1021-6.
Animal experiment: | Mice[1]C3H mice are used. LY 254155 is dosed on days 1, 4, 7, and 10 (4 treatment days). Cumulative dose is calculated using the formula (daily dose×number of treatment days). Doses are administered in mg of LY 254155 per kg of mouse weight (5, 10, 20, and 40 mg/kg), and 10 mice are inoculated at each dosing level, including a no-compound control group. % inhibition of tumor growth is calculated[1]. |
参考文献: [1]. Habeck LL, et al. A novel class of monoglutamated antifolates exhibits tight-binding inhibition of humanglycinamide ribonucleotide formyltransferase and potent activity against solid tumors. Cancer Res. 1994 Feb 15;54(4):1021-6. | |
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