Iadademstat (ORY-1001) 2HCl

Catalog No.S7795 Synonyms: RG-6016

For research use only.

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 No. 1431326-61-2

Selleck's Iadademstat (ORY-1001) 2HCl has been cited by 17 publications

Purity & Quality Control

Choose Selective Histone Demethylase Inhibitors

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 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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP1 M4XDPWZ2dmO2aX;uJIF{e2G7 MlL0NVMh\GG7cx?= MXrJcoR2[3Srb36gc4Yh\GmoZnXy[Y51cWG2aX;uJI9nKGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XO|ZYPz[YQh[XNiYXz0[ZJifGmxbjDpckBud3KyaH;sc4d6KG:oIHPvcI9vcWW|IHHmeIVzKDF|IHThfZMh[nliTXH5JGdzfW65YXzkMWdq\W2|YTDzeIFqdmmwZzDiZZNm\CCjc4PhfS=> NGDSSXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkewNlU1Oid-Mk[3NFI2PDJ:L3G+
THP1 NVTuZYJwTnWwY4Tpc44h[XO|YYm= NH\1WpIyOyCmYYnz MWTJcoR2[3Srb36gc4Yh\GmoZnXy[Y51cWG2aX;uJI9nKGi3bXHuJHRJWDFiY3XscJMh[W[2ZYKgNVMh\GG7czDifUBkgXSxc4DpckBie3OjeR?= NXrLdFQxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3NFI2PDJpPkK2O|AzPTR{PD;hQi=>
HCT116 MlnrR5l1d3SxeHnjbZR6KGG|c3H5 MVSyJJVO MnfMNVYhfG9iM{CgbJJ{ MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XRiMjD1UUBi\nSncjCxOkB1dyB|MDDodpMh[nlibXnjdo9{[2:yaXOgZY5idHm|aYO= M1G2d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO5PVE3Lz5{OUSzPVkyPjxxYU6=
PA1 Ml3iR5l1d3SxeHnjbZR6KGG|c3H5 M{n3XFIhfU1? MW[xOkB1dyB|MDDodpM> M3\MZ2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBCOSClZXzsd{BifCB{IIXNJIFnfGW{IEG2JJRwKDNyIHjyd{BjgSCvaXPyc5Nkd3CrYzDhcoFtgXOrcx?= NVLieXg2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|k6OTZpPkK5OFM6QTF4PD;hQi=>
F9 M{HwbmN6fG:2b4jpZ4l1gSCjc4PhfS=> NFLzTpMzKHWP MVqxOkB1dyB|MDDodpM> Mm\BR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgSlkh[2WubIOgZZQhOiC3TTDh[pRmeiBzNjD0c{A{OCCqcoOgZpkhdWmlcn;zZ49xcWNiYX7hcJl{cXN? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|OUmxOkc,Ojl2M{m5NVY9N2F-
Assay
Methods Test Index PMID
Growth inhibition assay Cell number 30568590
In vivo In rodent MV(4;11) xenografts, ORY-1001 (<0.020mg/kg, p.o.) leads to significantly reduced tumor growth. [1]

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: Rodent MV(4;11) xenografts
  • Dosages: <0.020mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 303.27
Formula

C15H22N. 2HCl

CAS No. 1431326-61-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(CCC1N)NC2CC2C3=CC=CC=C3.Cl.Cl

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

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Tech Support

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