TNP-351

TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Antifolate

Antifolate, DHFR[1]

TNP-351 inhibits the proliferation of mouse L1210 leukemia cells and human CCRF-CEM lymphoblastic leukemia cells with ED50 values of 0.79 and 2.7 nM, respectively[1]. The ED50 values determined for the parent cell line CCRF-CEM, CCRFCEM R30/6 subline, CCRF-CEM R1, and CCRF-CEM R2 are 2.7, 5.8, 94 and 76 nM, respectively[1]. Cell Viability Assay[1] Cell Line: L1210 and CCRF-CEM cells Concentration: 0.1, 0.3, 1, 3, and 10 nM for L1210 cells; 0.3, 1, 3, 10, and 30 for CCRF-CEM cells Incubation Time: 48 hours for L1210 cells; 72 hours for CCRF-CEM cells Result: The ED50 values were 0.79 and 2.7 nM for L1210 and CCRF-CEM cells, respectively.

[1]. F Itoh ,et al. Novel pyrrolo[2,3-d]pyrimidine Antifolate TNP-351: Cytotoxic Effect on Methotrexate-Resistant CCRF-CEM Cells and Inhibition of Transformylases of De Novo Purine Biosynthesis. Cancer Chemother Pharmacol. 1994;34(4):273-9.