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ORY-1001(trans) (Synonyms: ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride)

Catalog No.GC36818 Copy One-Click Copy Product Info

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

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ORY-1001(trans) Chemical Structure

Cas No.: 1431303-72-8

Size Price Stock Qty
10mM (in 1mL Water)
$158.00
In stock
5mg
$143.00
In stock
50mg
$784.00
In stock
100mg
$1,391.00
In stock

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Sample solution is provided at 25 µL, 10mM.



Description of ORY-1001(trans)

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

ORY-1001 trans is a KDM1A inhibitor that inactivate KDM1A by irreversible binding to the flavin adenine nucleotide (FAD) cofactor. ORY-1001 trans 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. ORY-1001 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 ORY-1001 trans[1].

ORY-1001 trans reduces AML tumor growth in mice and rat xenografts and increases survival time in a disseminated model of T-ALL[1].

[1]. Maes T, et al. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. Epigenomics. 2015;7(4):609-26. doi: 10.2217/epi.15.9.

Chemical Properties of ORY-1001(trans)

Cas No. 1431303-72-8 SDF
Synonyms ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride
Canonical SMILES N[C@@H]1CC[C@@H](N[C@H]2[C@H](C3=CC=CC=C3)C2)CC1.[H]Cl.[H]Cl
Formula C15H24Cl2N2 M.Wt 303.27
Solubility Water: 57.75 mg/mL (190.42 mM and warming); DMSO: 0.69 mg/mL (2.28 mM and warming) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of ORY-1001(trans)

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1 mg 5 mg 10 mg
1 mM 3.2974 mL 16.487 mL 32.9739 mL
5 mM 659.5 μL 3.2974 mL 6.5948 mL
10 mM 329.7 μL 1.6487 mL 3.2974 mL
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In vivo Formulation Calculator (Clear solution) of ORY-1001(trans)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Reviews

Review for ORY-1001(trans)

Average Rating: 5 ★★★★★ (Based on Reviews and 31 reference(s) in Google Scholar.)

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