Iadademstat (ORY-1001) is a highly potent, orally active and selective LSD1 (KDM1A) inhibitor with antileukemic activity. Iadademstat can be used for relapsed or refractory acute myeloid leukemia research
IC50&Target
LSD1
体外研究
Iadademstat (80-160 μM, 24 h-15 days) can inhibit the proliferation of cancer cells H1299 and A549, block the cell cycle in G1 phase, induce apoptosis, and inhibit the colony formation of H1299 and A549.
Iadademstat (80-160 μM, 24 h) reduced glycolysis in H1299 and A549 cells by lowering HK2 protein levels.
Cell Proliferation Assay
Cell Line:
H1299 and A549
Concentration:
80-160 μM
Incubation Time:
1-4 days
Result:
Inhibited cell proliferation.
WApoptosis Analysis
Cell Line:
H1299 and A549
Concentration:
80-160 μM
Incubation Time:
24 hours
Result:
Induced apoptosis.
Cell Cycle Analysis
Cell Line:
H1299 and A549
Concentration:
80-160 μM
Incubation Time:
48 hours
Result:
Arrested the cell cycle at G1 phase.
体内研究
Iadademstat (400 µg/kg, po, every 7 days for 28 days) showed anti-tumor activity in a glioblastoma xenograft mouse model.
Animal Model:
Glioblastoma xenograft mouse model
Dosage:
400 µg/kg
Administration:
po, every 7 days for 28 days
Result:
Inhibited the growth of tumors, increased the survival rate.
分子式
C15H22N2
分子量
230.35
CAS号
1431304-21-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 25 mg/mL (108.53 mM; ultrasonic and warming and heat to 60°C)