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    ORY-1001 (RG-6016) 2HCl
    ORY-1001 (RG-6016) 2HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0374
    CAS #: 1431326-61-2Purity ≥98%

    Description: ORY-1001 (RG-6016) is a novel, orally bioactive 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. 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.

    References: J Clin Oncol. 2013, 31, suppl; abstr. e13543.

    Related CAS #: 1431303-72-8 (2HCl)   1431304-21-0 (free base)   1431303-71-7 (xHCl)   1431326-61-2 (2HCl)  

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    Molecular Weight (MW)303.27
    FormulaC15H22N2 . 2HCl
    CAS No.1431326-61-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    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

    Synonyms

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


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    In 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.

    In VivoDaily 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 modelRodent MV(4;11) xenografts
    Formulation & Dosage<0.020mg/kg, p.o.
    References

    J Clin Oncol. 2013, 31, suppl; abstr. e13543.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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