Biological Activity
LTX-401 is an amphipathic amino-acid derivative for cytolytic cell-death and local tumor-immunology research. IC50 was 27 µM. This is a short-exposure cellular value, not a receptor-binding constant.
In Vitro
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| Cell viability | B16F1 melanoma; 4 h exposure. [1], Table 1 | IC50 was 27 µM. This is a short-exposure cellular value, not a receptor-binding constant. |
| Organelle response | B16F1 cells; 27 µM for 60 min. [1], Fig. 6 | Reduced LysoTracker signal indicated disruption of acidic organelle integrity. |
| Selectivity limitation | Normal endothelial cells, keratinocytes and fibroblasts. [1], Table 1 | LTX-401 also affected nonmalignant cells despite low hemolytic activity. The study does not support universal tumor-cell selectivity. |
In Vivo
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| Local tumor treatment | B16F1 melanoma in C57BL/6 mice; intratumoral 5 mg/mL solution once daily for 3 consecutive days. [1], Fig. 7 | Complete, lasting tumor regression occurred in 9 of 11 animals. The solution concentration is not a systemic mg/kg dose. |
Interpretation
The finding is specific to local treatment in the tested melanoma model and is not a universal cure rate.
