| Identification | Back Directory | [Name]
ORY-1001 | [CAS]
1431304-21-0 | [Synonyms]
ORY-1001 free base
ORY 1001 free base,ORY1001 free base
1,4-Cyclohexanediamine, N1-[(1R,2S)-2-phenylcyclopropyl]-, trans- | [Molecular Formula]
C15H22N2 | [MOL File]
1431304-21-0.mol | [Molecular Weight]
230.35 |
| Chemical Properties | Back Directory | [Boiling point ]
362.9±42.0 °C(Predicted) | [density ]
1.07±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
10.49±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
Iadademstat (400 μg/kg, po, every 7 days for 28 days) exhibits antitumor activity in glioblastoma xenograft mouse model[3]. | Animal Model: | Glioblastoma xenograft mouse model[3] | | Dosage: | 400 μg/kg | | Administration: | po, every 7 days for 28 days | | Result: | Inhibited the growth of tumors, increased the survival rate. |
| [IC 50]
LSD1 | [References]
[1] Olga Salamero, et al. First-in-Human Phase I Study of Iadademstat (ORY-1001): A First-in-Class Lysine-Specific Histone Demethylase 1A Inhibitor, in Relapsed or Refractory Acute Myeloid Leukemia. J Clin Oncol. 2020 Dec 20;38(36):4260-4273. DOI:10.1200/JCO.19.03250
[2] Lu Z, et al., ORY-1001 Suppresses Cell Growth and Induces Apoptosis in Lung Cancer Through Triggering HK2 Mediated Warburg Effect. Front Pharmacol. 2018 Dec 4;9:1411. DOI:10.3389/fphar.2018.01411
[3] Yang H, et al., [ORY-1001 inhibits glioblastoma cell growth by downregulating the Notch/HES1 pathway via suppressing lysine-specific demethylase 1 expression]. Nan Fang Yi Ke Da Xue Xue Bao. 2024 Aug 20;44(8):1620-1630. Chinese. DOI:10.12122/j.issn.1673-4254.2024.08.22 |
|
|