Iadademstat dihydrochloride

SKU: orb1301456

Description

Iadademstat dihydrochloride (ORY-1001) is a potent, selective, and covalent inhibitor of the epigenetic target KDM1A/LSD1. It is a research compound for studying acute leukemia, demonstrating activity in preclinical in vitro and in vivo models of the disease.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1431303-72-8
• MW: 303.27
• Purity: 99.78% (May vary between batches)
• Formula: C₁₅H₂₄Cl₂N₂
• SMILES: Cl.Cl.N[C@H]1CC[C@@H](CC1)N[C@@H]1C[C@H]1c1ccccc1
• Target: Histone Demethylase
• Solubility: PBS:100 mg/mL (329.74 mM);DMSO:3.04 mg/mL (10.02 mM)

Bioactivity

• In Vivo:
  ORY-1001 exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of an AML xenograft model, and extends survival in a mouse PDX (patient-derived xenograft) model of T cell acute leukemia. Surrogate pharmacodynamic biomarkers developed based on expression changes in leukemia cell lines were translated to samples from patients treated with ORY-1001. ORY-1001 is a selective KDM1A inhibitor in clinical trials and is currently being evaluated in patients with leukemia and solid tumors.
• In Vitro:
  ORY-1001 is a highly potent and selective KDM1A inhibitor that induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RG6016, RG-6016, RG 6016, RO7051790, RO-7051790, RO 7051790, inhibit, LSD1/KDM1A, ORY 1001, ORY1001, ORY-1001, ORY-1001(trans), HistoneDemethylase, Histone Demethylase, Inhibitor, Iadademstat, Iadademstat dihydrochloride, Iadademstat Dihydrochloride

Compound Identifiers

PubChem CID

71664305