biological activity | NCT-501 is an effective aldehyde dehydrogenase 1A1 (ALDH1A1) selective inhibitor of theophylline. the IC50 value is 40 nM when inhibiting hALDH1A1, which is more selective than other ALDH isozymes and other dehydrogenases (IC50 value> 57 UM when acting on hALDH1B1, hALDH3A1, and hALDH2). |
target | IC50: 40 nM (hALDH1A1) |
in vitro study | NCT-501 shows a 16% decrease in the Cal-27 CisR cell line at 20 nM concentration, though the difference was not statistically significant. |
in vivo study | NCT-501 (100 µg/animal; I. t.; every alternate day for 20 days) show a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts. Animal Model: 5-6 weeks old male Hsd: Athymic Nude-Foxn1nu (immuno-deficient-mice bearing Cal-27 CisR cells) Dosage: 100 µg/animal Administration: intra-tumorally (I .t); every alternate day for 20 days result: showa 78% inhibition in tumor growth in Cal-27 CisR derived xenografts. |
Animal Model:
| 5-6 weeks old male Hsd: Athymic Nude-Foxn1nu (immuno-deficient-mice bearing Cal-27 CisR cells) |
Dosage:
| 100µg/animal |
Administration:
| Intra-tumorally (i.t); every alternate day for 20 days |
Result:
| Showed a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts. |