Bioactivity | AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells[1]. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines[2]. |
Invitro | AMXT-1501 tetrahydrochloride (0.39-50 µM; 48 hours) treatment exhibits cytotoxicity against this panel of NB cell lines (BE(2)-C, SMS-KCNR and SH-SY5Y cells), with IC50 values of 17.72 µM for SMS-KCNR, 17.69 µM for BE(2)-C, and 14.13 µM for SH-SY5Y[2].BE(2)‐C, SMS‐KCNR and SH‐SY5Y cells are exposed to AMXT-1501 tetrahydrochloride (2.5 µM) and DFMO (2.5 mM) alone or in combination (AMXT-1501 tetrahydrochloride 2.5 µM + DFMO 2.5 mM). After 96 hours exposure to AMXT-1501 tetrahydrochloride or DFMO does not significantly alter the level of noncleaved PARP, cleaved PARP and cleaved caspase 3, whereas cells treated with the combination of AMXT-1501 tetrahydrochloride with DFMO decrease the amount of noncleaved PARP and increase the amount of cleaved PARP and cleaved caspase 3[2]. Cell Viability Assay[2] Cell Line: |
Name | AMXT-1501 tetrahydrochloride |
Formula | C32H72Cl4N6O2 |
Molar Mass | 714.77 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |