Iadademstat (ORY-1001; RG6016) 2HCl

Alias:

ORY1001; RG 6016;ORY-1001; RG-6016;ORY1001; RG6016; ORY1001 dihydrochloride, ORY1001 HCl; ORY1001 2HCl salt.

Cat No.:V0374 Purity: ≥98%
Iadademstat (ORY-1001; RG6016) 2HCl, the dihydrochloride salt of ORY1001, is a novel, orally bioactive and selective lysine-specific demethylase LSD1/KDM1A inhibitor with antineoplastic activity.
Iadademstat (ORY-1001; RG6016) 2HCl Chemical Structure CAS No.: 1431326-61-2
Product category: Histone Demethylase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Iadademstat (ORY-1001; RG6016) 2HCl, the dihydrochloride salt of ORY1001, is a novel, orally bioactive and selective lysine-specific demethylase LSD1/KDM1A inhibitor with antineoplastic activity. It inhibits LSD1/KDM1A with an IC50 of<20 nM, and shows high selectivity against related FAD dependent aminoxidases. ORY-1001 is an enantiomerically pure (trans conformation) KDM1A inhibitor. It exhibits excellent antiproliferative activity and high in vivo antitumor efficacy. ORY-1001 does not inhibit non-related histone modifiers, and is clean in a CEREP diversity panel. Treatment of THP-1 cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: In THP-1 (MLL-AF9) cells, ORY-1001 results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers. ORY-1001 also induces apoptosis in THP-1 and inhibits proliferation and colony formation of MV(4;11) (MLL-AF4) cells.


Kinase Assay: ORY-1001 (RG-6016) is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of<20 nM, with high selectivity against related FAD dependent aminoxidases. ORY-1001 is an enantiomerically pure KDM1A inhibitor with high selectivity against related FAD dependent aminoxidases. ORY-1001 does not inhibit non-related histone modifiers, and is clean in a CEREP diversity panel.


Cell Assay: ORY-1001 is an enantiomerically pure KDM1A inhibitor with high selectivity against related FAD dependent aminoxidases. ORY-1001 does not inhibit non-related histone modifiers, and is clean in a CEREP diversity panel. Treatment of THP-1 cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation at KDM1A target genes and concomitant induction of differentiation markers.

ln Vivo
Daily oral administration of doses < 0.020 mg/kg leads to significantly reduced tumor growth in rodent xenografts. In vivo studies have shown that ORY-1001 presents excellent oral bioavailability, target exposure and activity in vivo.
Animal Protocol
<0.020mg/kg, p.o.
Rodent MV(4;11) xenografts
References
J Clin Oncol. 2013, 31, suppl; abstr. e13543.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H22N2.2HCL
Molecular Weight
303.27
CAS #
1431326-61-2
SMILES
N(C1CCC(CC1)N)[C@@H]1C[C@H]1C1C=CC=CC=1.Cl.Cl
Synonyms

ORY1001; RG 6016;ORY-1001; RG-6016;ORY1001; RG6016; ORY1001 dihydrochloride, ORY1001 HCl; ORY1001 2HCl salt.

Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 5 mg/mL (16.5 mM)
Water:61 mg/mL (201.1 mM)
Ethanol:4 mg/mL warmed (13.2 mM)
Solubility (In Vivo)

Chemical Name:(1r,4R)-N1-((1R,2S)-2-phenylcyclopropyl)cyclohexane-1,4-diamine dihydrochloride

InChi Key:UCINOBZMLCREGM-ISDLZHGDSA-N

InChi Code: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

SMILES Code:N[C@@H]1CC[C@@H](N[C@@H]2C[C@H]2C3=CC=CC=C3)CC1.[H]Cl.[H]Cl

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.2974 mL 16.4870 mL 32.9739 mL
5 mM 0.6595 mL 3.2974 mL 6.5948 mL
10 mM 0.3297 mL 1.6487 mL 3.2974 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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