ORY-1001 structure
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Common Name | ORY-1001 | ||
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CAS Number | 1431304-21-0 | Molecular Weight | 286.375 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C17H22N2O2 | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of ORY-1001ORY-1001 (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases; exhibits low nanomolar cellular activity (EC50 < 1 nM) in the THP1 differentiation assay and induces the CD11b marker within 6 hr of treatment in FACS based differentiation assay in THP1 cell line; induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML; exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of AML xenograft models. |
Name | ORY-1001 |
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Description | ORY-1001 (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases; exhibits low nanomolar cellular activity (EC50 < 1 nM) in the THP1 differentiation assay and induces the CD11b marker within 6 hr of treatment in FACS based differentiation assay in THP1 cell line; induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML; exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of AML xenograft models. |
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References | 1. Maes T, et al. Cancer Cell. 2018 Mar 12;33(3):495-511.e12. |
Molecular Formula | C17H22N2O2 |
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Molecular Weight | 286.375 |