Name: Iadademstat (ORY-1001) 2HCl
Brand: Selleck Chemicals
SKU: S7795
Rating: 5 (21 reviews)

ORY-1001 (RG-6016) 2HCl 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. Phase 1.

Iadademstat (ORY-1001) 2HCl Chemical Structure

CAS: 1431326-61-2

Selleck's Iadademstat (ORY-1001) 2HCl has been cited by 21 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.95%

99.95

Iadademstat (ORY-1001) 2HCl Related Products

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Signaling Pathway

Histone Demethylase Signaling Pathway

Choose Selective Histone Demethylase Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
THP1	Function assay		13 days	Induction of differentiation of human THP1 cells assessed assessed as alteration in morphology of colonies after 13 days by May Grunwald-Giemsa staining based assay	26702542
THP1	Function assay		13 days	Induction of differentiation of human THP1 cells after 13 days by cytospin assay	26702542
HCT116	Cytotoxicity assay	2 uM	16 to 30 hrs	Cytotoxicity against human HCT116 cells at 2 uM after 16 to 30 hrs by microscopic analysis	29439916
PA1	Cytotoxicity assay	2 uM	16 to 30 hrs	Cytotoxicity against human PA1 cells at 2 uM after 16 to 30 hrs by microscopic analysis	29439916
F9	Cytotoxicity assay	2 uM	16 to 30 hrs	Cytotoxicity against mouse F9 cells at 2 uM after 16 to 30 hrs by microscopic analysis	29439916
Click to View More Cell Line Experimental Data

Biological Activity

Description

ORY-1001 (RG-6016) 2HCl 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. Phase 1.

Targets

LSD1 ^[1]

20 nM

In vitro
In vitro	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. ^[1]
Cell Research	Cell lines	NRK-52E cells
	Concentrations	10 μM
	Incubation Time	24 h
	Method	Cells treated with ORY-1001 (10 μM) for 24 h in the presence (vehicle) or TGF-β1.
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Growth inhibition assay	Cell number		30568590

In Vivo
In vivo	In rodent MV(4;11) xenografts, ORY-1001 (<0.020mg/kg, p.o.) leads to significantly reduced tumor growth. ^[1]
Animal Research	Animal Models	Rodent MV(4;11) xenografts
	Dosages	<0.020mg/kg
	Administration	p.o.

References

Chemical Information & Solubility

Molecular Weight	303.27	Formula	C₁₅H₂₂N₂. 2HCl
CAS No.	1431326-61-2	SDF	Download Iadademstat (ORY-1001) 2HCl SDF
Smiles	C1CC(CCC1N)NC2CC2C3=CC=CC=C3.Cl.Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

Water : 61 mg/mL

DMSO : 5 mg/mL ( (16.48 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

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 ddH₂O, 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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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