Name | T-3775440 hydrochloride |
Synonyms | T3775440 T 3775440 T-3775440HCl T-3775440 hydrochloride |
CAS | 1422535-52-1 |
EINECS | 604-604-1 |
Molecular Formula | C18H23ClN4O |
Molar Mass | 346.86 |
Storage Condition | Room Temprature |
In vitro study | T-3775440 enhances the transdifferentiation of erythrocytes/megakaryocytes into granulocyte-like monocytes. T-3775440 disrupts the interaction of LSD1 and GFI1B. AEL(TF-1a, HEL92.1.7) cells and AMKL(CMK11-5, M07e) cells were treated with T-3775440 for 48 hours, T-3775440 induced cell cycle arrest and apoptosis. In TF-1a and CMK11-5 cells, T-3775440 treatment increased G1 and sub-G1 cells. |
In vivo study | In the AML mouse xenograft model, T-3775440 inhibited tumor growth. In mice T-3775440 caused a transient decrease in platelets followed by a large rebound. After a single dose, T-3775440 had no significant effect on the number of red blood cells. In AEL(HEL 92.1.7) model and AMKL(CMK11-5) model, T-3775440 also exert anti-tumor activity. |
biological activity | T-3775440 HCl is an irreversible LSD1 inhibitor. It is highly selective for LSD1 relative to other monoamine oxidases with an IC50 of 2.1 nM. |
Target | Value |
LSD1 () | 2.1 nM |