Iadademstat dihydrochloride

Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.

Product information

CAS Number: 1431303-72-8

Molecular Weight: 303.27

Formula: C15H24Cl2N2

Chemical Name: (1r,4r)-N1-[(1R,2S)-2-phenylcyclopropyl]cyclohexane-1,4-diamine; bis(chlorohydrogen)

Smiles: Cl.Cl.N[C@@H]1CC[C@H](CC1)N[C@@H]1C[C@H]1C1C=CC=CC=1

InChiKey: UCINOBZMLCREGM-ISDLZHGDSA-N

InChi: InChI=1S/C15H22N2.2ClH/c16-12-6-8-13(9-7-12)17-15-10-14(15)11-4-2-1-3-5-11;;/h1-5,12-15,17H,6-10,16H2;2*1H/t12-,13-,14-,15+;;/m0../s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 0.69 mg/mL (2.28 mM; Need ultrasonic and warming). H2O : 57.75 mg/mL (190.42 mM; Need ultrasonic and warming).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Iadademstat dihydrochloride is a KDM1A inhibitor that inactivate KDM1A by irreversible binding to the flavin adenine nucleotide (FAD) cofactor. Iadademstat has very high selectivity for KDM1A over the MAO enzymes, high selectivity over KDM1B and unrivaled subnanomolar cellular activity in differentiation and colony formation assays on mixed lineage leukemia (MLL)-translocated acute myeloid leukemia (AML) cell lines. Iadademstat provokes a time and dose-dependent induction of the Cd11b differentiation marker in MLL-AF9 cells, which interestingly preceeds changes in H3K4me2 levels. While MLL-translocated cells are especially sensitive, other acute leukemia (AL) cell lines also respond to Iadademstat.

In Vivo:

Iadademstat reduces AML tumor growth in mice and rat xenografts and increases survival time in a disseminated model of T-ALL.

References:

1. Maes T , Mascaró, Cristina, Tirapu I , et al. ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia[J]. Cancer Cell, 2018:S1535610818300230.

Products are for research use only. Not for human use.