LSN 3213128 is a novel, potent, selective, nonclassical and orally bioavailable antifolate that inhibits Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase (AICARFT) with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. LSN-3213128 is highly effective in the suppression of tumor growth in a Cancer Xenograft Model. Inhibition of AICARFT with compound LSN-3213128 results in dramatic elevation of 5-aminoimidazole 4-carboxamide ribonucleotide (ZMP) and growth inhibition in NCI-H460 and MDA-MB-231met2 cancer cell lines. Treatment with this inhibitor in a murine based xenograft model of triple negative breast cancer (TNBC) resulted in tumor growth inhibition.
纯度:≥98%
CAS:1941211-99-9